kinase hinge binders · 2019. 11. 25. · hinge binders required for kinase atp-pocket inhibitors....

No 7, September 2013

Bellen Chemistry Co., Ltd. http://www.bellenchem.com

US contact: China contact: E-mail: [email protected] E-mail: [email protected]

Tel: 1-800-503-4529; 1-650-265-7852 / Fax: 1-650-240-2700 Tel: +86 10 89475061 / Fax: +86 10 89475062

Kinase Hinge Binders

Kinase inhibitors are a clinically important family of prescription drugs that belong to the class of so called

targeted therapy, for the treatment of cancer and more recently in the immunology area for the treatment of

arthritis. The ATP-binding pocket is located inside the deep cleft between the two lobes of the kinase

domains. The “hinge” is a single string of the amino acid segment that connects the two lobes. The

adenine ring of ATP binds to the hinge via two hydrogen bonds, one with the N-hydrogen and one with the

carbonyl group of the two amino acid residues located on the hinge. Of the 23 kinase inhibitors that have

reached the market so far (see Figure 1 below), all but two are kinase ATP-binding pocket inhibitors—they

form one to three hydrogen bonds to the amino acids of the hinge, thereby mimicking the hydrogen bonds that

are normally formed by the adenine ring of ATP.

Figure 1

In this issue of Bellen newsletter, we highlight some of Bellen’s novel building blocks that can be used as

hinge binders required for kinase ATP-pocket inhibitors. These hinge binders were designed carefully so

that they can form one to three hydrogen bonds to the hinge. They contain one to multiple functional groups

at various positions that can be derivatized sequentially. Additionally, the compounds with substituents such

as methyl, trfluoromethyl, methoxyl, or trifluoromethoxyl groups adjacent to the functional groups for the

purpose of conformation alteration are also available. We hope these compounds could spark some useful

ideas for your drug design.

In addition to the building blocks, we also provide a useful collection of library set consisting of thousands of

small heterocyclic compounds that can be used for fragment-based screening. Please contact us for details.

For a complete list of our catalog compounds, please visit Bellen’s website where you can do a structure

search. If you do not see the compound you need, please contact us at [email protected]. We

also provide custom synthesis for scales ranging from milligrams to tons.

mailto:[email protected]


Bellen Chemistry Co., Ltd. http://www.bellenchem.com US contact: China contact: E-mail: [email protected] E-mail: [email protected] Tel: 1-800-503-4529; 1-650-265-7852 / Fax: 1-650-240-2700 Tel: +86 10 89475061 / Fax: +86 10 89475062

1. Pyrozoles

HNN

CHO

Bellen000504

NN

CO2HMe

Bellen000543

NN

CHO

MeMe

Bellen001024

NN CO2H

Me

Bellen001483

NN CHO

Me

Bellen001534

NN

Me

MeBellen001830

NN

CHO

Bellen003154

NN

Me

Bellen003951

Me

NN

Me Cl.HCl

Bellen007399

NN

MeOH

Bellen001836

NN

Me

Br

Bellen007700

NN CHO

Me

Br

Bellen007702

HNN Br

Bellen008410

HNN CN

Br

Bellen001914

NN

B(OPIN)

Me

Me

Bellen006101

NN OHMe

Br

Bellen007701

Cl

CO2Me

NN OH

Br

Bellen007694

Me

NN CHO

Br

Bellen007692

Me

HNN

Me

Me

NH

NH2

Bellen008204

CO2HN

N

Me

Bellen002719

NN CO2H

Me

Me

Bellen004083

NN

CO2Me

Bellen006355

NH2N

NMe

Bellen009419

NN

NO2

Me Br

Bellen009704

NN OH

Bellen010958

NN NH2

MeBr

Bellen007414

NN

CHOMe

Bellen006087

HNN

NH2

Bellen000539

NN

CHO

Bellen000564

NHN

CO2Et

Me

Bellen012154

NN

ClBellen011832

NHN

OMe

Bellen011701

NH2NHN

Bellen010855

NH2

NN

Me

Bellen010479

OHNN

Me

Bellen009990

NN

CO2Me

Me

CHO

Bellen009812

HNN

CO2H

Bellen009721

HNN NH2

Bellen009291

NN

CO2HMe

NH2

Bellen009259

NN

NH2Me

Br

Bellen009251

HNN

Br

Br

Bellen009099

HNN

NH2

S

Bellen008243

NN

NH2

MeMe

Bellen008602

HNN

NO2

Br

Bellen009916

.HCl .HCl .HCl

.2HClOH

.HCl

NNNH

Bellen008295

NHNNH

Bellen005806

HN

NNH

Bellen005808

NHHNNH

Bellen005800

O

NHNNH

Bellen005807

.HCl

.HCl.HCl

Bellen011231

NNNH NN

NH BOC

F3C

Bellen011232Bellen011825

NHNNH

F3C

BOC.HCl

http://www.bellenchem.com/




2. Pyridines

CO2Me

NHMe

NH2N

Cl Br

Bellen007472

N

CO2HMe

Cl

Bellen007477

N CO2HMe

F

Bellen007480

NH2NMe

F

Bellen007481

NCl

MeO CO2H

Bellen007483

N CN

F Br

Bellen007488

N CO2H

F Br

NH2N

F Br

N

CO2HF

Cl


Bellen007490

N CN

MeBr

Bellen007494

N CO2H

MeBr

Bellen007498

NH2N

FCl

Bellen007497

NH2N

MeBr

Bellen007499

N

CO2HMe

ClBellen007501

N CN

Me Br

Bellen007503

N CO2H

Me Br

Bellen007504

NH2N

FBr

Bellen007506

N CO2H

F3C Cl

Bellen007507

N CN

F3C Cl

Bellen004081

NH2N

F3C Cl

Bellen001696

Bellen007508

N CN

MeCl

Bellen000630

OH

NMeN MeMe

Br

Bellen001388

N

CN

OMe

Cl

Bellen007514

CO2H

N OMe

Cl

Bellen007515

N

CHOF3C

Cl

Bellen007706N

CHOI

ClBellen000568

N

CHOI

FBellen001366

N

CHO

F

Br

Bellen004049

NCl

F NH2

Bellen007493

NH

HN

N

Bellen003801

Bellen008513

NH2N

F

Bellen008529

Bellen009163

N SO

O NH2

F3C

Bellen009436

N

HO

Bellen009832

N

OH

O

Bellen009954

N

NH2

NH

Ph

Bellen011009N CO2H

F

N

O

OHN

Bellen011125

Bellen011660N

NH2O

Bellen011692

N CO2H

F

F

Bellen011795

N

OH

F

F

Bellen011998

N F

F

Br

Bellen011999 Bellen012000 Bellen012001 Bellen012002Bellen012103 Bellen012104 Bellen012105

N F

F

CHO

N F

F

CO2H

N F

F

HO

N F

F

H2N

.HCl

N F

F

CN

N F

F

BocHN

N F

F

.2HCl

Bellen008514

NH2N

.2HClClNH2N .HCl

CF3

Bellen008672

NH2N

OMe.2HCl

.HCl

Bellen000710

NH2N

F3C

.HCl

Bellen000817

OHNBr

Bellen001373

N

CO2Et

NH2

Bellen001678

NHBocN

O2N

Bellen001695

NH2N

Me

Bellen001697

O

HNNH2N

Bellen003043

N

Br

Bellen003156

NNH

O O

OH

Bellen003383

O

NH

N

H2N

Bellen000431

N

O

NH2

NH2

Bellen000461

OHN

Br

Bellen000500

N

O2N

CO2H

Bellen000831

N

Bellen001751

N

Bellen005207

Br

N

O

Bellen008737N

Br

Bellen009918

N Br

Bellen009925

N

Br

Bellen010428

NH2

N

.HBr

.HBr.HBr .HCl .HBr

O

NH2

O

NHMe

.HCl .HCl

.HCl .HCl .HCl .HCl .HCl .HCl N

O

Bellen002773





3. Isoquinolines and Derivatives

N

CN

ClBellen002393

N

Cl

NC

Bellen002394

N

ClNC

Bellen002510

N

ClCN

Bellen002511

N

ClCN

Bellen003193

N

ClNC

Bellen003194

NNC

Cl

Bellen003195

N

CN

Cl

Bellen003196

N

NH2

Br

Bellen002183

Bellen002281

N

NH2

Br

Bellen002283

N

NH2Br

Bellen002451

Bellen002450

N

NH2

Br

N

NH2Br

Bellen002084

N

NH2

Br

Bellen008653

N

NH2

Br

Bellen009100

N

HO2C

Cl

Bellen002396

NHO2CCl

N

CO2HCl

Bellen003223

N

HO2C Cl

Bellen003224

NHO2C

Cl

Bellen003225

N

CO2H

Cl

Bellen003226

Bellen008915

N

ClCF3

N

F3C Cl

Bellen008916

NF3C

Cl

Bellen008917

N

CF3

Cl

Bellen008918

Bellen008911

N

CF3

Cl

N

F3C

Cl

Bellen008912

NF3CCl

Bellen008913

N

CF3 Cl


Bellen002942

N

N

N

Br

N

N

N

Cl

Bellen000717

N

N

N

Cl

Bellen006496

Bellen000090

N

O2N Cl

Bellen000091

N

ClBr

Bellen000597

N

Br

Br

Bellen000847

NBr

OH

Bellen001121

N

Cl

Br

Bellen001601

N

SO OCl

ClBellen001602

N

SO OCl

Me

Bellen001603

N

SO OCl

Br

Bellen001859

N

MeO

Cl

Bellen001995

NBr

Me

Bellen001996

N

MeBr

Bellen001997

N

Br Me

Bellen001998

N

NH2 Me

Bellen002280

N

Br

Cl

Bellen002285

NH

Br

O

Bellen002340

N

Cl

Br

Bellen002341

N

BrCl

Bellen002342

NBr

Cl

Bellen002383

N

Br

NH2

Bellen002395

N

CO2H

Cl

Bellen002448

N

Br

OH

Bellen002500

N

BrOH

Bellen002501

N

Br OH

Bellen002530

N

Br

Cl

Bellen002531

N

Br Cl

Bellen003202

N

OHC

Cl

Bellen003203

NOHCCl

Bellen003206

N

OHC Cl

Bellen003207

NO

Cl

Bellen003209

NH

CO2H

OBellen003210

NH

HO2C

O

Bellen003211

NHHO2CO

Bellen003222

N

HO2C Cl

Bellen003897

N

BrMe

Bellen005639

N

SO OCl

Me

Bellen006316

NH

O

NH2

Bellen007907

N

Cl

Br

Bellen008092

N

NH2

Bellen008201

N

H2NCl

Bellen008610

N

OMeBr

Bellen008611

N

OMe

Br

Bellen008612

N

OMeBr

Bellen009454

N

MeO2C

Cl

Bellen009455

NMeO2CCl

Bellen009776

N

CO2Me

Br

Bellen009777

N

MeBr

Bellen010041

N

H2N Cl

Bellen010042

NH2N

Cl

Bellen010115

N

OHCl

Bellen010296

NH

O

Br

Bellen010370

NH

ONH2

Bellen010500

N

MeO Cl

Bellen010984

N

Cl

Cl

Bellen011044

N

OHBr

Bellen011131

NHO

NH2

Bellen011237

N

CO2HMeO

Bellen011406

N

CHOCl

Bellen011532

N

MeO2C Cl

Bellen011590

N

ICl

Bellen011591

NMeOI

Bellen011592

N

IF

Bellen011711

NMeOCl

Bellen011754

NH

OF

Bellen011850

N

Me

Br

Bellen001551

NBr

Bellen000170

N

Br

Bellen003181

NH

CN

OBellen003182

NH

NC

O

Bellen010066

N

HO Cl

Bellen010067

NHO

Cl

Bellen010363

NH2NOMe

Bellen008252

N

NH2

Br

Bellen009780 Bellen009781

NClBr

Bellen009782

N

Cl Br

Bellen011597

NFBr

N

Cl

Br

Bellen006398

N

Cl Br

Bellen006399

N

ClBr

Bellen006400

NCl

Br

Bellen006404

N

Cl

Br

N

Br

NH2

Cl





4. Quinolines

Bellen000004

H2N

N

Bellen000388

N

NH2S

Bellen000391N

O NHNH2

Bellen000454N

NH2

Bellen000520

N

H2N S

Bellen000537

N

CN

Bellen002610

CO2H

N

Bellen002653

HO

N

Bellen002837

N Br

Bellen002839

NHO2C

Bellen002914

OHN

Bellen003718

NBr

Bellen003719

HO N

Bellen003791

NCN

Bellen003869

NH2

HN

NBellen005631

N

Bellen005671

N

SH

Bellen005672

NOHC

Bellen005692

N

CHO

Bellen006181

HO2C

N

Bellen008635

NH2N

Bellen008636

H2N N

Bellen009094

N

F

Bellen010683

N

EtO2C

Bellen011855

NNC

.HCl.HCl

.HCl

Bellen000224

NOMe

CO2H

Bellen000259

N

Br

Cl

Bellen000302

NOH

O2N

Bellen000578NCl

HN

Bellen000907

N Br

Bellen000908

N

Cl

Br

Bellen000909

N

Me

Br

Bellen000987

NNH2

Bellen002346

N

Br

OMe

Bellen003436

N

BrCl

Bellen004111

NBr Br

Bellen005645

NCHO

Br

Bellen005995

N

CO2H

CF3

Bellen008096N

ClCl

Bellen008180

AcO

N

Br

Bellen008440

N

BrBzlO

Bellen008794

N

NH2Br

Bellen008795

N

H2N Br

Bellen008796

NH2N

Br

Bellen008797

NNH2

Br

Bellen008798

N

CO2HBr

Bellen008799

N

Br

Bellen008800

NHO2C

Br

Bellen008801

NCO2H

Br

Bellen009087

N CF3

Br

Bellen009088

N

OHH2N

Bellen009090

NMe

Br

Bellen009092

N

H2NBr

Bellen009093

NOH

Br

Bellen009095

N

Cl

Br

Bellen009230

N

N

N

CO2H

Bellen009319

NMe

Cl

Bellen010530

N

CO2H

Me

Bellen010866

NH

Br

O

Bellen011225N

O

F

Bellen011226N

IF

Bellen011633

N

OHBr

Bellen011671

N

CNOH

Bellen012086

N

OH

F

Bellen012200

N

Cl

Br

Me

HO2C

NH2





5. Quinazolines and Pyridopyrazines

Bellen009023

HN

NH

O

O

MeO

MeO

Bellen000761

N

NH

F

O

Bellen000778

N

NClCl

Cl

Bellen001101

N

N

F

Bellen001939

HN

NCl

O

Bellen002770

N

N

Cl

CO2Et

Bellen003802

N

N

Cl

Cl

Bellen006168

N

N

Cl

Cl

Cl

Bellen006216

N

NMeOCl

Cl

Bellen006221

N

NFCl

Cl

Bellen006224

N

N

F

Cl

Cl

Bellen006225

N

N

F

Cl

Cl

Bellen007861

N

N

NH2

Bellen007898

N

NH

O

Me

Bellen011241

N

N

IBellen004008

N

N

Cl

N

N N

Br

Bellen003001

N

N

N

MeBr

Bellen009034

N

N

N

Bellen006256

Bellen000608

N

N N

NH2

Bellen001406

N

N

N

Br

Bellen001530

N

N N Br

Bellen001826

N

N N

I

Bellen001982

N

N

HO2C

N

Bellen009889

N

N

N

F

Cl

Bellen002039

N

N N

OMe

Bellen002456

N

N N Cl

Bellen002809

N

N N

Br

Bellen002819

Bellen002908

N

N N

OMe

N

N N

NO2

Bellen002951

N

N

N

OMe

Bellen003020

N

NN

OMe

Bellen003024

N

N N OMe

Bellen011120

NN

NCl

ClBellen002942

N

N

N

Br

N

N

N

Cl

Bellen000717

N

N

N

Cl

Bellen006496





6. Indazoles

Bellen000117

NH

NBr

CO2Me

Bellen000232

NH

NBr

Cl

Bellen000250

NN

Br

BOC

Bellen000331

NN

Br

BOC

Bellen000332

NN

BrBOC

Bellen000726

NH

N

I

Br

Bellen000727

NH

NBr

I

Bellen000800

NH

NF

Br

Bellen000801

NH

NF

Br

Bellen001002

NH

N

MeO2C Br

Bellen001554

NH

N

Br Cl

Bellen001561

NH

NBr

CO2H

Bellen001625

NH

NBr

CO2Et

Bellen001755

NH

NBr

CO2Et

Bellen002040

NH

NBr

CN

Bellen002049

NH

NBr

OMe

Bellen002148

NH

NMeO

Br

Bellen003722

NH

NBr

Me

Bellen003723

NH

N

Br

Me

Bellen003725

NH

N

Br

Me

Bellen003726

NH

N

BrMe

Bellen003972

NH

N

Cl Br

Bellen007712

NH

NF

Br

Bellen008454

NH

NF

Br

Bellen008807

NH

NCF3O

Br

Bellen008878

NH

N

OMe

Br

Bellen009424

NH

N

CO2H

Br

Bellen009450

NH

NF3C

Br

Bellen009914

NH

NEtO

Br

Bellen009915

NH

NO

Br

Bellen010130

NH

N

OMe

Br

Bellen010255

NH

N

CO2Me

Br

Bellen010608

NH

N

F

Br

Bellen010625

NH

NF3CO

Br

Bellen010632

NH

NMeO2C

Br

Bellen010633

NH

NMeO2C

Br

Bellen010634

NH

NMeO

Br

NH

N

B(OPIN)


NN

(HO)2B

Bellen004715

NH

NPINO

Bellen000529

NN

PINO

Bellen003429

NH

N(PINO)B

Bellen000530

NH

N

MeBr

Bellen000056

NH

N

Me

Br

Bellen000471

NH

NMe

Br

Bellen001720

NH

N

MeBr

Bellen001934

NH

NBr

Bellen002043

NH

N

MeBr

Bellen002057

NH

NMe

Br

Bellen002151

NH

NMe

Br

Bellen002168

NH

N

Me

Br

Bellen003051

NH

N

B(OH)2Me

Bellen003779

NN

BrMe

BOC

Bellen003798

NN

MeBr

BOC

Bellen006516

NNH

BOC

O

Br

Bellen007720

NH

N

IF

Br

Bellen007721

NH

NF

Br

Br

Bellen007722

NH

NF

Cl

Br

Me

NH

N

B(OH)2

Bellen000713

NH

N

(HO)2B

Bellen002169

Me

NH

N

B(OH)2

Bellen002171

Me NH

N

B(OH)2

Bellen002172Me

NN

B(OH)2

THPBellen000971

NH

N(HO)2B

Bellen000002

NH

N(HO)2B

Me

Bellen002173

NH

N(HO)2B

Me

Bellen002174

NN

(HO)2B

Bellen004029

THP BOC

NH

N(HO)2B

Me

Bellen002175

Me

THPNH

N(HO)2B

OMe


NH

N(HO)2B

Bellen010133

NH

N(HO)2B

MeOOMe

NN

(HO)2B

Bellen004024

NH

N(HO)2B

Bellen000003

NH

N(HO)2B

Me

Bellen002177

NH

N(HO)2B

F

Bellen007717

THP

NH

N(HO)2B

Me

Bellen002059

NN

(HO)2B

Me

Bellen004059

THPNH

N(HO)2B

MeO

Bellen009457

NH

N(HO)2B

EtO

Bellen009666

NH

N(HO)2B

i-PrO

Bellen009667

NH

N(HO)2B

O

Bellen009668

NH

N(HO)2B

CF3

Bellen009772

NH

N(HO)2B

CF3O

Bellen009669

NH

N

Bellen007056

(HO)2BNH

N

Bellen000462

(PINO)BNH

N

Bellen010135(HO)2B

OMe

Bellen00017

NN

BrF

BOCBellen007721

NH

NF

Br

Bellen003239

NH

N

Br

H2N

Bellen003238

NH

N

BrH2N

Bellen003240

NH

N

Br

H2NBellen003237

NH

N

BrH2N

NH

N

Br

Bellen003690

Me

Bellen002909

NH

N

Br

Br

NH

N

NH2Br

Bellen002801

NH

N

ClBr

Bellen000055

Bellen010129

NN

BrOMe

BOCBellen001553

NH

NBr

CO2H

Bellen003839

NH

NBr

CO2Me

Bellen002020

NH

N

NH2

Br

Bellen009239

NH

N

CN

Br

Bellen010131

NH

NBr

OMe

Bellen007715

NN

F

BrBOC

Bellen007718

NN

F

BrTHP

Bellen000021

NH

N

Br

Cl

Bellen000211

NH

N

Br

Bellen010132

NH

N

BrMeO

Bellen004361

NH

N

Br

OMe

Bellen000018

NH

NCl

I

Bellen007751

NH

NI

CO2H

Bellen000018

NH

NCl

I

NH

N

IH2N

Bellen002464

NH

N

IMeO2C


NH

NOHC

Cl

Br





7. Azaindazoles

N NNH

Br

Bellen003245

N NNH

Br

Bellen003269

N NNH

Br

Bellen003268

NN

NH

Br

Bellen002101

Bellen006003

NCl

NH

N

Bellen009381

N NNH

Cl

Bellen009330

NN

NHBr

Bellen009331

NN

NH

Br

Bellen009332

N NNH

Br

Bellen009333

N NNHBr

Bellen009335

N NNH

Br

Bellen009338

NN

NHBr

Br

Bellen009341

NN

NH

I

Br

Bellen009339

NN

NH

BrBr

Bellen009343

NN

NHBr

Br

Bellen009344

N NNHBr

Br

Bellen009345

N NNH

Br Br

Bellen009346

N NNH

I

BrBellen009347

N NNH

I

Br

Bellen009348

N NNH

IBr

Bellen009350

N NNH

BrBr

Bellen009352

N NNH

I

BrBellen009353

N NNH

IBr

Bellen009361

NN

NHCl

Bellen009362

NN

NH

Cl

Bellen009363

N NNH

Cl

Bellen009364

N NNHCl

Bellen009365

N NNH

Cl

Bellen009367

N NNH

Cl

Bellen009368

N NNH

Cl

Bellen009370

N NNH

Cl

Bellen009374

NN

NHCl

Br

Bellen009375

NN

NH

ClBr

Bellen009378

NN

NH

ICl

Bellen009379

N NNH

Cl

Br

Bellen009380

N NNHCl

Br

Bellen009381

N NNH

Cl Br

Bellen009382

N NNH

I

ClBellen009383

N NNH

I

Cl

Bellen009384

N NNH

ICl

Bellen009386

N NNH

ClBr

Bellen009388

N NNH

I

ClBellen009389

N NNH

ICl

Bellen009400

N NNH

Bellen009403

N NNH

OMe

Bellen009404

N NNH

MeO

Bellen009405

N NNH

OMe

Br

Bellen009406

N NNH

MeOBr

Bellen009413

N NNH

NH2

Bellen009931

N NNH

Br

Bellen010164

NN

NH

Bellen010168

N NNH

NN

NH

Br

Bellen002016

NN

NH

Bellen009336

NN

NH

Bellen003431

Br

NN

NH

Bellen003432

Cl

NN

NH

Bellen003433

I

NN

NH

Bellen005043

CHO

NN

NH

Bellen005501

NH2

NN

NH

Br

Bellen003270

Bellen003430

N

ClN

NH

Bellen006152

NN

NH

NH2Br

Bellen009372

NN

NH

Cl

Bellen009392

NN

NH

ClBr

Bellen009393

NN

NH

Cl Br

Bellen009059

NN

NH

IBr

Bellen010170

N NNH

Bellen010166

N NNH

Bellen010162

NN

NH

Bellen010160

NN

NH

Bellen010176

N NNH

Bellen010174

N NNH

Bellen010172

N NNH

Bellen010177

N NNH

Bellen010175

N NNH

Bellen010173

N NNH

Bellen010165

NN

NH

Bellen010163

NN

NH

Bellen010161

NN

NH

NN

NH

NH2

Bellen009411

Bellen009395

NN

NH

MeO

Bellen009396

NN

NH

OMe

OMe

Bellen009366

N NNH

Cl

Bellen009360

NN

NH

Cl

Bellen010071

N NNH

MeO2C

Bellen010070

NN

NH

MeO2C

Bellen009329

NN

NH

Br

Bellen009373

NN

NH

Cl

Br

Bellen009397

NN

NH

BrMeO

Bellen009387

N NNH

BrCl

Bellen009385

N NNH

Br

Cl

Bellen009398

NN

NH

OMe

Br

Bellen009351

N NNH

Br Br

Bellen009342

NN

NH

IBr

Bellen009349

N NNH

Br

Br

Bellen009337

NN

NH

Br

Br

Bellen009376

NN

NH

Cl

I

Bellen009354

N NNH

Br I

Bellen010169

N NNH

Bellen010171

N NNH

Bellen010167

N NNH

Bellen009399

N NNHMeO

Bellen009414

NN

NHBr

NH2

Bellen008189

N NNH

Br

Br

Bellen009402

N NNH

OMe Br

Bellen009401

N NNH

Br

MeO

Bellen009391

NN

NH

Br

Cl

Bellen009410

NN

NH

OMe Br

Bellen009409

NN

NH

Br

MeO NN

NH

Bellen009357

Br Br

NN

NH

Br

Bellen009356

Br

BrN

NNH

Bellen009355

Br

Bellen005044

NN

NH

CO2HBr

Br

NN

NH

Bellen009358

Br

I

NN

NH

Bellen009371

ClN

NNH

Bellen009394

Cl

I

Bellen009061

N

ClN

NH

I

NN

NH

Bellen009407

MeO

NN

NH

Bellen009408

OMe

NN

NH

Bellen010182

NN

NH

Bellen010180

NN

NH

Bellen010183

NN

NH

Bellen010181

NN

NH

Bellen003433

F

N

N NNH

Bellen006457

NH2

N

N NNH

Bellen001257

Cl

N

N NNH

Bellen001201

Cl

N

N NNH

Bellen002348

Cl

Cl

N

N NNH

Bellen002843

H2N

Cl Me

N

N NNH

Bellen002778

H2N

ClBr

N

N NNH

Bellen002767

H2N

Cl Br

N

N NNH

Bellen002817

H2N

ClI

N

N NNH

Bellen002798H2N

Cl

I

N

N NNH

Bellen002859

H2N

Cl

N

N NNH

Bellen002889

H2N

Cl

OH

N

N NNH

Bellen002820

H2N

ClI

N

N NNH

Bellen006446

Cl

NH2

N

N NNH

Bellen002781

H2N

OMe

N

HN NNH

Bellen006445

Cl

O





8. Azaindoles, Azabenzimidazoles and Other Heterocycles

N NH

NMe

Br

Bellen009036

NBr

N

NH

Bellen003064

N

N

NH

Bellen010675

Bellen008064

N

B(OPIN)

NH

Bellen000472

N NH

I

Bellen000646

N NH

O

NH2

Bellen001249

N NH

Br

Bellen001593

Bellen001941

N NH

CO2Me

Bellen001958

NCl

NH2

NH

Bellen002222

NCl NH

CO2H

Bellen003916

N

Cl

NH

I

Bellen003918

N

Cl

NH

I

Bellen003919

N

Cl

NH

Br

Bellen004842

N NH

CO2H

Bellen005934

N NH

CO2Me

Bellen001599

Bellen007745

N NTs

Br

Bellen007797

N NH

CHO

Bellen007915

N NH

FBr

Bellen007973

N NH

CHO

Bellen008429

N NBOC

Cl

Bellen008507

Bellen008595

N NH

Cl

Bellen008889

Bellen003295

N

Cl

NH

Bellen005843

N

Br

NH

Bellen006001

N

Cl

NH

.HCl

N NH

NH2

Bellen001958

NCl

NH2

NH

Bellen003073

N

NH2

NH

Bellen001959

N

MeO

NH

Br

N

Br

NH

Bellen010490

N

Br

NH

Cl

Bellen007579

N NHBr

Bellen005141

N

Br

NH

CO2H

Bellen002424

N

ICl

NH N

NCCl

NH

N

HO2CCl

NH

Bellen005025

N NHCl

Bellen002022

N NH

CO2Et

Bellen004138

N NH

CHO

Bellen000240

N

OMe

NH

N

N NH

Bellen006150

N

N NH

Bellen002731

BrBr

N

N NH

Bellen002797

BrCl NH2

HN

N NH

Bellen002775

BrO

N

N NH

Bellen002695

NH2

N

N NH

Bellen000285

Cl

N

N NH

Bellen006010

ClN

N NH

Bellen001541

Cl

Cl

N

N NH

Bellen002716

Cl

H2N

N

N NH

Bellen012881

Cl

Cl

CO2MeN

N NH

Bellen009747

I

N

N NH

Bellen002696

Cl I

Cl

HN

N NH

Bellen002782

O I N

N NH

Br N

N NH

IBr

N

N

NH

Br

Bellen002923

Br

Me

N

N

NH

Br

Bellen010671

Me

N NH

NMe

Br

Bellen010668

Me NBr

N

NH

Bellen010770

Me

N

N

NH

Bellen010674

Cl

MeN

N

NH

Cl

Bellen009030

N

N

NH

Bellen012884

H2N

NH

O

Bellen002803

Br

NH

O

Bellen001567

Br

NH

O

Bellen001795

Br NH

O

Bellen006424

BrNH

O

Bellen009714

(PINO)B

NH

O

Bellen010075

NH2

NH

O

Bellen003040

HO2C

NH

Bellen002786

MeO2C

NH

O

Bellen007904

Me2OC

NH

O

Bellen008548

HO

NH

O

Bellen000493

HO NH

O

Bellen008741

F3C HN

NH

Br

Bellen002986

O

HN

NH

(PINO)B

Bellen003316

O

Bellen001986

N

N

Br N

NH

.2HCl

.2HCl


NN

NH

Bellen010892

O2N NN

NH

Bellen002953

Br

Br





9. Isosteres of Quinolines and Quinazolines

N

OOHC

Bellen011801

N

OHO2C

Bellen011804

N

O

Bellen011807

NOOHC

Bellen011802

NOHO2C

Bellen011805

NO

Bellen011808

N

O

Cl

Bellen007760

NO

Br

Bellen010256

N

S

H2N

Bellen001217

NS ClBr

Bellen001932

N

SEtO2C

H2N

Bellen002154

NS

H2N

Bellen001195

NSRO2C

R-Me: Bellen003300R=Et: Bellen001931

H2N

N

S

Bellen007170

OH

N

S

Bellen005855

ClH2N

H2N

Bellen004060

N

S

O2N

Bellen012012

MeHN

NS

Bellen012111

NSHO

N

SHO2C

H2N

Bellen008634

N

NS

Bellen005457

NH2

N

NS

Bellen004482

Cl

N

N

HN

Bellen009145

Cl

N

N

HN

Bellen009241

Cl

Cl

N

HN

H2N

Bellen001266

N

S

Bellen001929

Cl

Cl

Bellen007759

N

O

Br

N

HN

OHC

Bellen008030

N

HN

Bellen005125

OHCN

HN

R=H: Bellen007544R=Et: Bellen011746

RO2C

N

HN

HO2C

Bellen005126

N

HN

Bellen008036

H2N

N

HN

Br

Bellen000957

N

HN

Bellen001188

HO2COMe N

HN

Br

Bellen002288

OMeN

HN

Br

Bellen007909

Cl

N

HN

Bellen001188

OMe

Bellen011745

HO

N

HN





10. Isosteres of Isoquinolines

NO

OHC

Bellen011803

NO

HO2C

Bellen011806

NO

Cl

Bellen005846

NS

OHC

Bellen003642

NS

HO2C

Bellen011812

NS

Bellen011815

NS

Bellen0011811

NSHO2C

Bellen011813

NS

Bellen011814

NS

RO2C

R=H: Bellen003249R=Me: Bellen010409

NS

Cl

Br

Bellen000451

NSMeO2C

Br

Bellen001026

NSEtO2C

H2N

Bellen001930

NSMeO2C

Me

Bellen002298

NS

H2N

Bellen000627

NS

Br

Bellen000168

NS

Bellen001838

Br

NS

Bellen001244

Br

NO

Bellen011809

NS

Bellen011810

NSOHC

Bellen002292

OHC

OHC

Bellen003253

NS

HO2CN

S

H2N

Bellen001205

NS

Bellen003251

Bellen003255

NS

Bellen002985

H2N

H2N

H2N

H2N

H2N

NHS

O

Br

NS

Bellen000168

NC

NS

Bellen002292

OHC

Me

NS

Bellen003247

NS

Bellen002298

H2N

NS

Bellen002291

OHC

Cl

NS

Bellen001928

EtO2C

H2N

NS

Bellen003252

NC

NS

Bellen003642

Cl

H2N

NS

Bellen005828Cl

Br

Bellen002826

N

HN

NBr

Bellen002869

N

BrHN

N

Bellen002911

N

BrHN

N

Bellen010667

NNH

NMe

Br

Bellen010669

NNH

NMe

Cl

Bellen010745

NN

HN Cl

Cl

NN

HN

Cl

Bellen006497

NNH

N Cl

Bellen000716

.HCl

Bellen003254

NS

HO

Bellen00xxxx

N

HN

NBr

Me

Bellen001287

N

HN

H2N

Bellen012118

HO

NNH

Bellen000179

N

HN

OHC

Bellen000460

N

OMe

NH

HO2C

Bellen000958

N

HN

Br

Bellen002209

N

ClHN

HO2C

Bellen002286

N

OMe

NH

Br

Bellen003685

N

HN

Cl

Bellen005920

NNH

EtO2C

ClBellen006265

NNH

EtO2COMe

Bellen007542

NNH

HO2C

Bellen007798

NNH

OHC

Bellen007910

N

HN Cl

Bellen007911

N

HN Cl

Br

Bellen007912

N

HN

ClBr

Bellen007916

NNH

Cl

Br

Bellen008032

NNH

OHC

Bellen000179

N

HNHO

Bellen003255

N

HN

H2N

Bellen00xxxx

NNH

H2N

Bellen00xxxx

NNH

Br

Bellen00xxxx

N

OBzl

NH

MeO2C

O

H2N

HO





11. Imidazopyridines, Imidazopyrazines,Triazolopyridines and Triazolopyrazines

NN

Br

F

Bellen003409

NN

Br

Bellen004321

N N

NMe

Br

Bellen006491

NN

O2N

Br

Bellen007817

N N

NMe

Br

Bellen006490

N N

N

Me

Br

Bellen006489

N NN

Br

Bellen006268

N N

NBr

Bellen006332

N N

NBr

Bellen003911

N N

N

Br

Bellen001407

N N

N

Br

Bellen003729

NN

CO2H

Bellen008404

NN

ClBr

Bellen003923

NN

Me

Br

Bellen003921

NN

CO2HMe

Me

Bellen003720

NN

Cl

Bellen003046

NN

CO2H

Me

Bellen002743

NN

Br

Bellen002532

NN

Br

Bellen002481

NNBr

Bellen002338

NN

Cl

Br

Bellen001039

NN

CO2Et

MeCl

Bellen000113

NN

Br

NH2

Bellen003349

NN

Br

Me

Bellen009125

NN N

Br

Bellen001210

NN N

Br

Br

Bellen001983

NN N

NH2

Br

Bellen001985

NN N

Cl

Bellen001990

NN N

Cl

Br

Bellen001991

NN N

N

CO2Et

Bellen003528

NN N

Br

Bellen005725

NN N

Cl

Bellen005738

NN N

NCl

Bellen006242

NN N

Cl

Bellen007581

NN N

NC

Bellen007582

NN N

NH2

Bellen007584

NN N

Me

Br

Bellen007586

NN N

Me Br

Bellen007587

NN N

MeOBr

Bellen007589

NN N

ClBr

Bellen007591

NN N

OMe

Br

Bellen007592

NN N

Cl Br

Bellen007593

NN N

MeBr

Bellen008498

NN N

NOMe

BrN

N NN

Cl

Br


NN N

N

Cl

Bellen009049

NN N

NOMe

Br

Bellen009050

NN N

N

Cl

Bellen009051

NN N

N

Me

Cl

Bellen009052

NN N

N

CF3

Cl

Bellen009053

.HCl

Bellen001993

NN

N

Br

OMe

Bellen007590

NN N

OMe Br

Bellen009011

NN N

Me

Br

Bellen009858

NN N

Bellen000220

N N NN

ClCl

Bellen000574

N N NN

Cl

Bellen002435

N N NN

ClMe

Bellen003369

N N NN

Me

OCl

NN

NNH2

Br

NN

NNH2

Br

NN

NNH2

Cl

NN

NNH2

Br

F

NN

NNH2

ClN

N

NNH2

Br

NN

NNH2

Br

NN

NNH2

CO2MeN

N

NNH2

MeO2CN

N

NNH2

MeO2C

NN

NNH2

CO2Me

NN

NNH2

ClN

N

NNH2

Cl

NN

NNH2

F3C

Br

NN

NNH2

Br

Cl

NN

NNH2

Br

Me

NN

NNH2

Br

I

NN

NNH2

CN

NN

NNH2

Br

MeO2C


Bellen012383


Bellen012385 Bellen012386 Bellen012387

Bellen009509 Bellen009498 Bellen009506Bellen009505

Bellen012388

Bellen012391

Bellen012392Bellen012393Bellen012394

Bellen012395

Bellen012396

.HCl



kinase hinge binders · 2019. 11. 25. · hinge binders required for kinase atp-pocket inhibitors....

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