General Information of the Protein
Protein ID
PT00876
Protein Name
Tyrosine-protein kinase Lck
Secondarily
Protein Name
Leukocyte C-terminal Src kinase
Lymphocyte cell-specific protein-tyrosine kinase
Protein YT16
Proto-oncogene Lck
T cell-specific protein-tyrosine kinase
p56-LCK
Gene Name
LCK
Sequence
MGCGCSSHPEDDWMENIDVCENCHYPIVPLDGKGTLLIRNGSEVRDPLVTYEGSNPPASPLQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKANSLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKHYKIRNLDNGGFYISPRITFPGLHELVRHYTNASDGLCTRLSRPCQTQKPQKPWWEDEWEVPRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNYIHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKERPEDRPTFDYLRSVLEDFFTATEGQYQPQP
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Src family
Function
Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells. Plays a key role in T-cell antigen receptor (TCR)-linked signal transduction pathways. Constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors. Association of the TCR with a peptide antigen-bound MHC complex facilitates the interaction of CD4 and CD8 with MHC class II and class I molecules, respectively, thereby recruiting the associated LCK protein to the vicinity of the TCR/CD3 complex. LCK then phosphorylates tyrosine residues within the immunoreceptor tyrosine-based activation motifs (ITAM) of the cytoplasmic tails of the TCR-gamma chains and CD3 subunits, initiating the TCR/CD3 signaling pathway. Once stimulated, the TCR recruits the tyrosine kinase ZAP70, that becomes phosphorylated and activated by LCK. Following this, a large number of signaling molecules are recruited, ultimately leading to lymphokine production. LCK also contributes to signaling by other receptor molecules. Associates directly with the cytoplasmic tail of CD2, which leads to hyperphosphorylation and activation of LCK. Also plays a role in the IL2 receptor-linked signaling pathway that controls the T-cell proliferative response. Binding of IL2 to its receptor results in increased activity of LCK. Is expressed at all stages of thymocyte development and is required for the regulation of maturation events that are governed by both pre-TCR and mature alpha beta TCR. Phosphorylates other substrates including RUNX3, PTK2B/PYK2, the microtubule-associated protein MAPT, RHOH or TYROBP. Interacts with FYB2 (PubMed:27335501).
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Uniprot ID
Primary ID:
P06239

Secondarily ID:
D3DPP8
P07100
Q12850
Q13152
Q5TDH8
Q5TDH9
Q7RTZ3
Q96DW4
Q9NYT8
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Ensembl ID
ENSG00000182866
HGNC ID
HGNC:6524
Subcellular Location
Cell membrane
Cytoplasm
Cytosol
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0065873
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone
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C26H29N7O2
 1
1
GI50 = 310 nM
   TI
   LI
   LO
   TS
CP0190068
N-[4-methyl-3-[1-(6-methylpyridine-3-carbonyl)piperidin-4-yl]oxyphenyl]-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C33H38F3N5O3
 1
1
GI50 = 386 nM
   TI
   LI
   LO
   TS
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0147351
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)benzamide
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C31H30F3N9O
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0147359
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(4-ethylpiperazin-1-yl)-5-(trifluoromethyl)benzamide
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C32H32F3N9O
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0309083
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-5-tert-butylthiophene-2-carboxamide
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C27H27N7OS
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0150295
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-chloro-4-[(4-ethylpiperazin-1-yl)methyl]benzamide
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C32H34ClN9O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0485534
2-(4-(6-(6-(2-(2-chloro-6-methylphenylamino)-1H-benzo[d]imidazol-1-yl)pyrimidin-4-ylamino)-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol
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C29H31ClN10O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0166375
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C26H20F3N7O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0230192
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(1-methylpiperidin-4-yl)oxy-5-(trifluoromethyl)benzamide
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C32H31F3N8O2
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0268699
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-tert-butylpyridine-4-carboxamide
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C28H28N8O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0309066
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-isopropylphenyl)-4-methylbenzamide
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C28H27N7O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0327702
4-N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]-2-methyl-6-N-(2-morpholin-4-ylethyl)pyrimidine-4,6-diamine
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C29H31ClN10O
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0166378
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)benzamide
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C30H24F3N9O
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0147352
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-tert-butylphenyl)-4-methylbenzamide
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C29H29N7O
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0199004
N-(2-chloro-6-methylphenyl)-1-[6-[[4-(morpholin-4-ylmethyl)pyridin-2-yl]amino]pyrimidin-4-yl]benzimidazol-2-amine
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C28H27ClN8O
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0289191
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-1-tert-butyl-5-[(4-methylpiperazin-1-yl)methyl]pyrazole-3-carboxamide
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C32H39N11O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0136623
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
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C26H20F3N7O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0147357
4-methyl-3-(1-(4-(3-(4-methylpiperazin-1-yl)propylamino)-1,3,5-triazin-2-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
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C33H35F3N10O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0278790
4-methyl-3-(1-(6-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
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C34H36F3N9O
 1
1
IC50 = 23 nM
   TI
   LI
   LO
   TS
CP0289193
N-[4-methyl-3-[[1-[6-[3-(4-methylpiperazin-1-yl)propylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C34H36F3N9O
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0166283
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-methylbenzamide
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C26H23N7O
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0327707
N-(2-chloro-6-methylphenyl)-1-[6-[[5-(2-morpholin-4-ylethyl)pyridin-2-yl]amino]pyrimidin-4-yl]benzimidazol-2-amine
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C29H29ClN8O
 1
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0166281
3-(1-(6-(4-(dimethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
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C32H33F3N8O
 1
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0227163
N-[4-methyl-3-[[1-[6-(3-morpholin-3-ylpropylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C33H33F3N8O2
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0227161
N-[3-[[1-[6-[4-(diethylamino)butylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C34H37F3N8O
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0150292
4-methyl-3-(1-(6-(2-(4-methylpiperazin-1-yl)ethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
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C33H34F3N9O
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0230191
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(difluoromethoxy)phenyl)-4-methylbenzamide
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C26H21F2N7O2
 1
1
IC50 = 47 nM
   TI
   LI
   LO
   TS
CP0166376
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-5-cyclopropyl-1H-pyrazole-3-carboxamide
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C25H23N9O
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0147354
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-bromophenyl)-4-methylbenzamide
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C25H20BrN7O
 1
1
IC50 = 52 nM
   TI
   LI
   LO
   TS
CP0150291
3-(1-(6-(4-(diethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
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C34H37F3N8O
 1
1
IC50 = 52 nM
   TI
   LI
   LO
   TS
CP0294208
N-[4-methyl-3-[[1-[6-[2-(4-methylpiperazin-1-yl)ethylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C33H34F3N9O
 1
1
IC50 = 56 nM
   TI
   LI
   LO
   TS
CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0166371
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-chlorophenyl)-4-methylbenzamide
   Show/Hide
C25H20ClN7O
 1
1
IC50 = 76 nM
   TI
   LI
   LO
   TS
CP0290251
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-m-tolylbenzamide
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C26H23N7O
 1
1
IC50 = 83 nM
   TI
   LI
   LO
   TS
CP0290298
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-chlorobenzamide
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C25H20ClN7O
 1
1
IC50 = 84 nM
   TI
   LI
   LO
   TS
CP0166278
N-[3-[[1-[6-[4-(dimethylamino)butylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C32H33F3N8O
 1
1
IC50 = 108 nM
   TI
   LI
   LO
   TS
CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
   Show/Hide
C17H18N4O2
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0151357
N-[3-[[1-[6-(2-methoxyethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C29H26F3N7O2
 1
1
IC50 = 132 nM
   TI
   LI
   LO
   TS
CP0166372
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-methoxyphenyl)-4-methylbenzamide
   Show/Hide
C26H23N7O2
 1
1
IC50 = 157 nM
   TI
   LI
   LO
   TS
CP0151356
N-[4-methyl-3-[[1-[6-(2-pyridin-2-ylethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C33H27F3N8O
 1
1
IC50 = 171 nM
   TI
   LI
   LO
   TS
CP0166284
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-5-tert-butyl-2-methylpyrazole-3-carboxamide
   Show/Hide
C27H29N9O
 1
1
IC50 = 224 nM
   TI
   LI
   LO
   TS
CP0268700
N-[3-[[1-[6-(2-hydroxyethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C28H24F3N7O2
 1
1
IC50 = 229 nM
   TI
   LI
   LO
   TS
CP0289528
N-[4-methyl-3-[[1-[6-(2-pyrrolidin-2-ylethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H31F3N8O
 1
1
IC50 = 238 nM
   TI
   LI
   LO
   TS
CP0181870
3-(1-(6-(2-cyanoethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C29H23F3N8O
 1
1
IC50 = 275 nM
   TI
   LI
   LO
   TS
CP0166374
4-methyl-3-(1-(6-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-m-tolylbenzamide
   Show/Hide
C34H39N9O
 1
1
IC50 = 337 nM
   TI
   LI
   LO
   TS
CP0138730
4-N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]-5-methyl-6-N-(2-morpholin-4-ylethyl)pyrimidine-4,6-diamine
   Show/Hide
C29H31ClN10O
 1
1
IC50 = 359 nM
   TI
   LI
   LO
   TS
CP0358252
N-[3-[[1-[6-(4-aminobutylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C30H29F3N8O
 1
1
IC50 = 366 nM
   TI
   LI
   LO
   TS
CP0289196
N-[3-[[1-[6-(3-aminopropylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C29H27F3N8O
 1
1
IC50 = 387 nM
   TI
   LI
   LO
   TS
CP0289530
N-[3-[[1-[6-[(4-aminocyclohexyl)amino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H31F3N8O
 1
1
IC50 = 392 nM
   TI
   LI
   LO
   TS
CP0166280
3-(1-(6-(4-(diethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-m-tolylbenzamide
   Show/Hide
C34H40N8O
 1
1
IC50 = 406 nM
   TI
   LI
   LO
   TS
CP0298947
N-[3-[[1-[6-[2-(diethylamino)ethylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H33F3N8O
 1
1
IC50 = 418 nM
   TI
   LI
   LO
   TS
CP0158669
1-(6-aminopyrimidin-4-yl)-N-(2-chloro-6-methylphenyl)-1H-benzo[d]imidazol-2-amine
   Show/Hide
C18H15ClN6
 1
1
IC50 = 438 nM
   TI
   LI
   LO
   TS
CP0166285
N-[3-[[1-[6-(2-aminoethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C28H25F3N8O
 1
1
IC50 = 470 nM
   TI
   LI
   LO
   TS
CP0166379
3-(1-(6-(4-(dimethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-m-tolylbenzamide
   Show/Hide
C32H36N8O
 1
1
IC50 = 531 nM
   TI
   LI
   LO
   TS
CP0399208
1-(6-aminopyrimidin-4-yl)-N-mesityl-1H-benzo[d]imidazol-2-amine
   Show/Hide
C20H20N6
 1
1
IC50 = 583 nM
   TI
   LI
   LO
   TS
CP0166279
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(2-methylpyridin-4-yl)benzamide
   Show/Hide
C25H22N8O
 1
1
IC50 = 702 nM
   TI
   LI
   LO
   TS
CP0150285
4-methyl-3-(1-(6-(2-(4-methylpiperazin-1-yl)ethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-m-tolylbenzamide
   Show/Hide
C33H37N9O
 1
1
IC50 = 762 nM
   TI
   LI
   LO
   TS
CP0150281
N-[4-methyl-3-[[1-[6-[(1-methylpiperidin-4-yl)amino]pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H31F3N8O
 1
1
IC50 = 881 nM
   TI
   LI
   LO
   TS
CP0166277
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-chloropyridine-4-carboxamide
   Show/Hide
C24H19ClN8O
 1
1
IC50 = 890 nM
   TI
   LI
   LO
   TS
CP0147358
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3,5-dichlorobenzamide
   Show/Hide
C25H19Cl2N7O
 1
1
IC50 = 1074 nM
   TI
   LI
   LO
   TS
CP0316983
1-(6-aminopyrimidin-4-yl)-N-(2-bromo-4,6-dimethylphenyl)-1H-benzo[d]imidazol-2-amine
   Show/Hide
C19H17BrN6
 1
1
IC50 = 1167 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
   Show/Hide
C23H26N6O3S
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
   Show/Hide
C20H15N5
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0269791
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-phenylbenzamide
   Show/Hide
C25H21N7O
 1
1
IC50 = 2280 nM
   TI
   LI
   LO
   TS
CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
   Show/Hide
C28H32N6O5
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0289192
N-[3-[[1-(6-chloropyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C26H18ClF3N6O
 1
1
IC50 = 2702 nM
   TI
   LI
   LO
   TS
CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
   Show/Hide
C27H28FN7O2
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0166373
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(isoquinolin-5-yl)-4-methylbenzamide
   Show/Hide
C28H22N8O
 1
1
IC50 = 3241 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
   Show/Hide
C22H25FN6O2
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0166282
3-(1-(6-amino-5-methylpyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C27H22F3N7O
 1
1
IC50 = 4456 nM
   TI
   LI
   LO
   TS
CP0158276
N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]-N',N'-diethylbutane-1,4-diamine
   Show/Hide
C26H32ClN7
 1
1
IC50 = 5036 nM
   TI
   LI
   LO
   TS
CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
   Show/Hide
C26H27FN6O
 1
1
IC50 = 5200 nM
   TI
   LI
   LO
   TS
CP0288253
N-(2-chloro-6-methylphenyl)-1-(6-chloropyrimidin-4-yl)benzimidazol-2-amine
   Show/Hide
C18H13Cl2N5
 1
1
IC50 = 5704 nM
   TI
   LI
   LO
   TS
CP0178078
N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]morpholin-4-amine
   Show/Hide
C22H22ClN7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0316985
N-(2-chloro-6-methylphenyl)-1-(6-morpholin-4-ylpyrimidin-4-yl)benzimidazol-2-amine
   Show/Hide
C22H21ClN6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0147360
N-[4-methyl-3-[[1-(6-morpholin-4-ylpyrimidin-4-yl)benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C30H26F3N7O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0166377
N-[3-[[1-(6-methoxypyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C27H21F3N6O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0281287
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-carbamoylphenyl)-4-methylbenzamide
   Show/Hide
C26H22N8O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0005166
BMS-354825
   Show/Hide
C22H26ClN7O2S
 7
1 IC50 = 0.4 nM
2 IC50 < 1 nM
3 IC50 < 1.5 nM
4 IC50 = 2.3 nM
5 IC50 = 3 nM
6 IC50 = 4 nM
7 Kd = 0.2 nM
CP0031719
(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
   Show/Hide
C21H22Cl2FN5O
 3
1 IC50 < 1 nM
2 IC50 = 2741 nM
3 Kd = 30 nM
CP0027166
1-(tert-butyl)-3-(4-chlorophenyl)-4-aminopyrazolo[3,4-d]pyrimidine
   Show/Hide
C15H16ClN5
 2
1 IC50 = 4 nM
2 Ki = 0.7943 nM
CP0150295
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-chloro-4-[(4-ethylpiperazin-1-yl)methyl]benzamide
   Show/Hide
C32H34ClN9O
 1
1 IC50 = 4 nM
CP0125726
N-[4-[7-amino-3-[3-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]-3-cyclopentylpropanamide
   Show/Hide
C31H37N7O
 1
1 IC50 = 4 nM
CP0158792
N-[4-[7-amino-3-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]-3-cyclopentylpropanamide
   Show/Hide
C31H37N7O
 1
1 IC50 = 4 nM
CP0327702
4-N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]-2-methyl-6-N-(2-morpholin-4-ylethyl)pyrimidine-4,6-diamine
   Show/Hide
C29H31ClN10O
 1
1 IC50 = 5 nM
CP0166278
N-[3-[[1-[6-[4-(dimethylamino)butylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H33F3N8O
 1
1 IC50 = 5 nM
CP0232583
1-(4-(7-amino-3-(4-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)-3-(cyclohexylmethyl)urea
   Show/Hide
C31H38N8O
 1
1 IC50 = 5 nM
CP0289193
N-[4-methyl-3-[[1-[6-[3-(4-methylpiperazin-1-yl)propylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C34H36F3N9O
 1
1 IC50 = 6 nM
CP0165977
1-(4-(7-amino-3-(3-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)-3-(cyclohexylmethyl)urea
   Show/Hide
C31H38N8O
 1
1 IC50 = 6 nM
CP0036779
9-(2,6-dimethylphenyl)-4-[4-(4-methylpiperazin-1-yl)anilino]-1,3,5,9,11-pentazatetracyclo[8.7.0.02,7.012,17]heptadeca-2,4,6,10,12,14,16-heptaen-8-one
   Show/Hide
C31H30N8O
 1
1 IC50 = 7 nM
CP0289191
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-1-tert-butyl-5-[(4-methylpiperazin-1-yl)methyl]pyrazole-3-carboxamide
   Show/Hide
C32H39N11O
 1
1 IC50 = 8 nM
CP0093636
1-(4-(7-amino-3-(3-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)-3-(2-chlorophenyl)urea
   Show/Hide
C30H29ClN8O
 1
1 IC50 = 8 nM
CP0105352
3-(4-(7-amino-3-(3-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)-1-cyclohexyl-1-methylurea
   Show/Hide
C31H38N8O
 1
1 IC50 = 8 nM
CP0268699
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-tert-butylpyridine-4-carboxamide
   Show/Hide
C28H28N8O
 1
1 IC50 = 10 nM
CP0147351
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)benzamide
   Show/Hide
C31H30F3N9O
 1
1 IC50 = 11 nM
CP0147359
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(4-ethylpiperazin-1-yl)-5-(trifluoromethyl)benzamide
   Show/Hide
C32H32F3N9O
 1
1 IC50 = 11 nM
CP0150292
4-methyl-3-(1-(6-(2-(4-methylpiperazin-1-yl)ethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C33H34F3N9O
 1
1 IC50 = 11 nM
CP0166375
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C26H20F3N7O
 1
1 IC50 = 11 nM
CP0147357
4-methyl-3-(1-(4-(3-(4-methylpiperazin-1-yl)propylamino)-1,3,5-triazin-2-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C33H35F3N10O
 1
1 IC50 = 12 nM
CP0227161
N-[3-[[1-[6-[4-(diethylamino)butylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C34H37F3N8O
 1
1 IC50 = 12 nM
CP0358252
N-[3-[[1-[6-(4-aminobutylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C30H29F3N8O
 1
1 IC50 = 13 nM
CP0299320
3-(4-(7-amino-3-(4-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)-1-cyclohexyl-1-methylurea
   Show/Hide
C31H38N8O
 1
1 IC50 = 13 nM
CP0199004
N-(2-chloro-6-methylphenyl)-1-[6-[[4-(morpholin-4-ylmethyl)pyridin-2-yl]amino]pyrimidin-4-yl]benzimidazol-2-amine
   Show/Hide
C28H27ClN8O
 1
1 IC50 = 14 nM
CP0232582
phenyl N-[4-[7-amino-3-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
   Show/Hide
C30H29N7O2
 1
1 IC50 = 14 nM
CP0166281
3-(1-(6-(4-(dimethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C32H33F3N8O
 1
1 IC50 = 15 nM
CP0191400
phenyl N-[4-[7-amino-3-[3-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
   Show/Hide
C30H29N7O2
 1
1 IC50 = 16 nM
CP0116325
DAMNACANTHAL
   Show/Hide
C16H10O5
 2
1 IC50 = 17 nM
2 IC50 = 620 nM
CP0230191
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(difluoromethoxy)phenyl)-4-methylbenzamide
   Show/Hide
C26H21F2N7O2
 1
1 IC50 = 17 nM
CP0150291
3-(1-(6-(4-(diethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C34H37F3N8O
 1
1 IC50 = 18 nM
CP0278790
4-methyl-3-(1-(6-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C34H36F3N9O
 1
1 IC50 = 18 nM
CP0166374
4-methyl-3-(1-(6-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-m-tolylbenzamide
   Show/Hide
C34H39N9O
 1
1 IC50 = 19 nM
CP0166280
3-(1-(6-(4-(diethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-m-tolylbenzamide
   Show/Hide
C34H40N8O
 1
1 IC50 = 20 nM
CP0147352
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-tert-butylphenyl)-4-methylbenzamide
   Show/Hide
C29H29N7O
 1
1 IC50 = 22 nM
CP0166379
3-(1-(6-(4-(dimethylamino)butylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-m-tolylbenzamide
   Show/Hide
C32H36N8O
 1
1 IC50 = 22 nM
CP0026727
2-methylpropyl N-[4-[7-amino-3-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
   Show/Hide
C28H33N7O2
 1
1 IC50 = 22 nM
CP0289196
N-[3-[[1-[6-(3-aminopropylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C29H27F3N8O
 1
1 IC50 = 23 nM
CP0232561
N-[4-[7-amino-3-[3-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]-4-(trifluoromethyl)benzamide
   Show/Hide
C31H28F3N7O
 1
1 IC50 = 23 nM
CP0230192
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(1-methylpiperidin-4-yl)oxy-5-(trifluoromethyl)benzamide
   Show/Hide
C32H31F3N8O2
 1
1 IC50 = 24 nM
CP0232562
2-methylpropyl N-[4-[7-amino-3-[3-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
   Show/Hide
C28H33N7O2
 1
1 IC50 = 24 nM
CP0485534
2-(4-(6-(6-(2-(2-chloro-6-methylphenylamino)-1H-benzo[d]imidazol-1-yl)pyrimidin-4-ylamino)-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol
   Show/Hide
C29H31ClN10O
 1
1 IC50 = 25 nM
CP0165979
1-(4-(7-amino-3-(4-(4-methylpiperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)-3-(2-chlorophenyl)urea
   Show/Hide
C30H29ClN8O
 1
1 IC50 = 25 nM
CP0227163
N-[4-methyl-3-[[1-[6-(3-morpholin-3-ylpropylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C33H33F3N8O2
 1
1 IC50 = 26 nM
CP0268700
N-[3-[[1-[6-(2-hydroxyethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C28H24F3N7O2
 1
1 IC50 = 27 nM
CP0294208
N-[4-methyl-3-[[1-[6-[2-(4-methylpiperazin-1-yl)ethylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C33H34F3N9O
 1
1 IC50 = 29 nM
CP0309066
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-isopropylphenyl)-4-methylbenzamide
   Show/Hide
C28H27N7O
 1
1 IC50 = 30 nM
CP0327707
N-(2-chloro-6-methylphenyl)-1-[6-[[5-(2-morpholin-4-ylethyl)pyridin-2-yl]amino]pyrimidin-4-yl]benzimidazol-2-amine
   Show/Hide
C29H29ClN8O
 1
1 IC50 = 31 nM
CP0150285
4-methyl-3-(1-(6-(2-(4-methylpiperazin-1-yl)ethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-m-tolylbenzamide
   Show/Hide
C33H37N9O
 1
1 IC50 = 38 nM
CP0289528
N-[4-methyl-3-[[1-[6-(2-pyrrolidin-2-ylethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H31F3N8O
 1
1 IC50 = 38 nM
CP0147354
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-bromophenyl)-4-methylbenzamide
   Show/Hide
C25H20BrN7O
 1
1 IC50 = 43 nM
CP0309083
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-5-tert-butylthiophene-2-carboxamide
   Show/Hide
C27H27N7OS
 1
1 IC50 = 43 nM
CP0290251
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-m-tolylbenzamide
   Show/Hide
C26H23N7O
 1
1 IC50 = 52 nM
CP0147358
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3,5-dichlorobenzamide
   Show/Hide
C25H19Cl2N7O
 1
1 IC50 = 58 nM
CP0136623
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
   Show/Hide
C26H20F3N7O
 1
1 IC50 = 59 nM
CP0166371
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-chlorophenyl)-4-methylbenzamide
   Show/Hide
C25H20ClN7O
 1
1 IC50 = 63 nM
CP0166283
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-methylbenzamide
   Show/Hide
C26H23N7O
 1
1 IC50 = 70 nM
CP0289530
CHEMBL1076473
   Show/Hide
C32H31F3N8O
 1
1 IC50 = 71 nM
CP0158793
N-[4-[7-amino-3-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]-4-(trifluoromethyl)benzamide
   Show/Hide
C31H28F3N7O
 1
1 IC50 = 75 nM
CP0024455
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide
   Show/Hide
C26H32N6O2
 1
1 IC50 = 88 nM
CP0166372
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-methoxyphenyl)-4-methylbenzamide
   Show/Hide
C26H23N7O2
 1
1 IC50 = 90 nM
CP0002230
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
   Show/Hide
C28H22F3N7O
 2
1 IC50 = 108.2 nM
2 Kd = 47 nM
CP0298947
N-[3-[[1-[6-[2-(diethylamino)ethylamino]pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C32H33F3N8O
 1
1 IC50 = 111 nM
CP0138730
4-N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]-5-methyl-6-N-(2-morpholin-4-ylethyl)pyrimidine-4,6-diamine
   Show/Hide
C29H31ClN10O
 1
1 IC50 = 119 nM
CP0166376
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-5-cyclopropyl-1H-pyrazole-3-carboxamide
   Show/Hide
C25H23N9O
 1
1 IC50 = 120 nM
CP0290298
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-chlorobenzamide
   Show/Hide
C25H20ClN7O
 1
1 IC50 = 132 nM
CP0151357
N-[3-[[1-[6-(2-methoxyethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C29H26F3N7O2
 1
1 IC50 = 135 nM
CP0029878
1-tert-butyl-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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C16H19N5
 3
1 IC50 = 151 nM
2 IC50 = 250 nM
3 Ki = 63.1 nM
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 5
1 IC50 = 160 nM
2 IC50 = 320 nM
3 Kd = 39.81 nM
4 Kd = 40 nM
5 Kd = 62 nM
CP0150281
N-[4-methyl-3-[[1-[6-[(1-methylpiperidin-4-yl)amino]pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C32H31F3N8O
 1
1 IC50 = 168 nM
CP0166279
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(2-methylpyridin-4-yl)benzamide
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C25H22N8O
 1
1 IC50 = 177 nM
CP0151356
N-[4-methyl-3-[[1-[6-(2-pyridin-2-ylethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C33H27F3N8O
 1
1 IC50 = 204 nM
CP0166285
N-[3-[[1-[6-(2-aminoethylamino)pyrimidin-4-yl]benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C28H25F3N8O
 1
1 IC50 = 230 nM
CP0166378
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)benzamide
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C30H24F3N9O
 1
1 IC50 = 238 nM
CP0166284
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-5-tert-butyl-2-methylpyrazole-3-carboxamide
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C27H29N9O
 1
1 IC50 = 316 nM
CP0746969
(6,7-Dimethoxy-quinazolin-4-yl)-(3,4,5-trimethoxy-phenyl)-amine hydrochloride
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C19H22ClN3O5
 1
1 IC50 = 500 nM
CP0158669
1-(6-aminopyrimidin-4-yl)-N-(2-chloro-6-methylphenyl)-1H-benzo[d]imidazol-2-amine
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C18H15ClN6
 1
1 IC50 = 514 nM
CP0166373
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(isoquinolin-5-yl)-4-methylbenzamide
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C28H22N8O
 1
1 IC50 = 616 nM
CP0166277
N-[3-[[1-(6-aminopyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-chloropyridine-4-carboxamide
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C24H19ClN8O
 1
1 IC50 = 715 nM
CP0158276
N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]-N',N'-diethylbutane-1,4-diamine
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C26H32ClN7
 1
1 IC50 = 789 nM
CP0269791
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-phenylbenzamide
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C25H21N7O
 1
1 IC50 = 1080 nM
CP0289192
N-[3-[[1-(6-chloropyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C26H18ClF3N6O
 1
1 IC50 = 1162 nM
CP0316983
1-(6-aminopyrimidin-4-yl)-N-(2-bromo-4,6-dimethylphenyl)-1H-benzo[d]imidazol-2-amine
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C19H17BrN6
 1
1 IC50 = 1355 nM
CP0181870
3-(1-(6-(2-cyanoethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
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C29H23F3N8O
 1
1 IC50 = 1367 nM
CP0399208
1-(6-aminopyrimidin-4-yl)-N-mesityl-1H-benzo[d]imidazol-2-amine
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C20H20N6
 1
1 IC50 = 1785 nM
CP0166377
N-[3-[[1-(6-methoxypyrimidin-4-yl)benzimidazol-2-yl]amino]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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C27H21F3N6O2
 1
1 IC50 = 2030 nM
CP0166282
3-(1-(6-amino-5-methylpyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
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C27H22F3N7O
 1
1 IC50 = 2400 nM
CP0178078
N-[6-[2-(2-chloro-6-methylanilino)benzimidazol-1-yl]pyrimidin-4-yl]morpholin-4-amine
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C22H22ClN7O
 1
1 IC50 > 2500 nM
CP0288253
N-(2-chloro-6-methylphenyl)-1-(6-chloropyrimidin-4-yl)benzimidazol-2-amine
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C18H13Cl2N5
 1
1 IC50 > 2500 nM
CP0316985
N-(2-chloro-6-methylphenyl)-1-(6-morpholin-4-ylpyrimidin-4-yl)benzimidazol-2-amine
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C22H21ClN6O
 1
1 IC50 > 2500 nM
CP0147360
N-[4-methyl-3-[[1-(6-morpholin-4-ylpyrimidin-4-yl)benzimidazol-2-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C30H26F3N7O2
 1
1 IC50 > 2500 nM
CP0281287
3-(1-(6-aminopyrimidin-4-yl)-1H-benzo[d]imidazol-2-ylamino)-N-(3-carbamoylphenyl)-4-methylbenzamide
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C26H22N8O2
 1
1 IC50 > 2500 nM
CP0722826
(6,7-Dimethoxy-quinazolin-4-yl)-methyl-phenyl-amine hydrochloride, 0.8 M EtOH
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C17H18ClN3O2
 1
1 IC50 > 100000 nM
CP0080103
2-{4-[2-[1-(4-Methoxy-benzyl)-4-methyl-2-oxo-1,2-dihydro-pyridin-3-ylcarbamoyl]-2-(2-methyl-2-naphthalen-2-yl-propionylamino)-ethyl]-phenyl}-2-methyl-propionic acid
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C41H43N3O6
 1
1 Kd = 1000 nM
Clinical Information about the Protein
Target 1 ( LCK tyrosine protein kinase (LCK) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Chronic myelogenous leukaemia [ICD-11: 2A20.0]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Gram-positive bacterial infection [ICD-11: 1B74-1G40]
Approved Drug(s) 1 Approved Drug  1
1 Dasatinib Approved
Chronic myelogenous leukaemia
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 VX-680 Phase 2
Solid tumour/cancer
Investigative Drug(s) 2 Investigative Drugs  2
1 GW-788388 Investigative
Solid tumour/cancer
2 HKI-9924129 Investigative
Gram-positive bacterial infection