General Information of the Protein
Protein ID
PT01314
Protein Name
Tyrosine-protein kinase ITK/TSK
Secondarily
Protein Name
Interleukin-2-inducible T-cell kinase
Kinase EMT
T-cell-specific kinase
Tyrosine-protein kinase Lyk
Gene Name
ITK
Secondarily
Gene Name
EMT
LYK
Sequence
MNNFILLEEQLIKKSQQKRRTSPSNFKVRFFVLTKASLAYFEDRHGKKRTLKGSIELSRIKCVEIVKSDISIPCHYKYPFQVVHDNYLLYVFAPDRESRQRWVLALKEETRNNNSLVPKYHPNFWMDGKWRCCSQLEKLATGCAQYDPTKNASKKPLPPTPEDNRRPLWEPEETVVIALYDYQTNDPQELALRRNEEYCLLDSSEIHWWRVQDRNGHEGYVPSSYLVEKSPNNLETYEWYNKSISRDKAEKLLLDTGKEGAFMVRDSRTAGTYTVSVFTKAVVSENNPCIKHYHIKETNDNPKRYYVAEKYVFDSIPLLINYHQHNGGGLVTRLRYPVCFGRQKAPVTAGLRYGKWVIDPSELTFVQEIGSGQFGLVHLGYWLNKDKVAIKTIREGAMSEEDFIEEAEVMMKLSHPKLVQLYGVCLEQAPICLVFEFMEHGCLSDYLRTQRGLFAAETLLGMCLDVCEGMAYLEEACVIHRDLAARNCLVGENQVIKVSDFGMTRFVLDDQYTSSTGTKFPVKWASPEVFSFSRYSSKSDVWSFGVLMWEVFSEGKIPYENRSNSEVVEDISTGFRLYKPRLASTHVYQIMNHCWKERPEDRPAFSRLLRQLAEIAESGL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Tec family
Function
Tyrosine kinase that plays an essential role in regulation of the adaptive immune response. Regulates the development, function and differentiation of conventional T-cells and nonconventional NKT-cells. When antigen presenting cells (APC) activate T-cell receptor (TCR), a series of phosphorylation lead to the recruitment of ITK to the cell membrane, in the vicinity of the stimulated TCR receptor, where it is phosphorylated by LCK. Phosphorylation leads to ITK autophosphorylation and full activation. Once activated, phosphorylates PLCG1, leading to the activation of this lipase and subsequent cleavage of its substrates. In turn, the endoplasmic reticulum releases calcium in the cytoplasm and the nuclear activator of activated T-cells (NFAT) translocates into the nucleus to perform its transcriptional duty. Phosphorylates 2 essential adapter proteins: the linker for activation of T-cells/LAT protein and LCP2. Then, a large number of signaling molecules such as VAV1 are recruited and ultimately lead to lymphokine production, T-cell proliferation and differentiation (PubMed:12186560, PubMed:12682224, PubMed:21725281). Required for TCR-mediated calcium response in gamma-delta T-cells, may also be involved in the modulation of the transcriptomic signature in the Vgamma2-positive subset of immature gamma-delta T-cells (By similarity). Phosphorylates TBX21 at 'Tyr-530' and mediates its interaction with GATA3 (By similarity).
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Uniprot ID
Primary ID:
Q08881

Secondarily ID:
B2R752
Q32ML7
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HGNC ID
HGNC:6171
Subcellular Location
Cytoplasm
Nucleus
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: CL000302 , DT40
Compound ID Compound Name Compound Formula
CP0043199
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H23N7O3S
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0035804
(R)-N-(5-(((3,3-dimethylbutan-2-yl)(methyl)amino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H36N6O2S
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0035801
(S)-N-(5-(((3,3-dimethylbutan-2-yl)(methyl)amino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H36N6O2S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0071438
(R)-N-(5-((3,3-dimethylbutan-2-ylamino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H34N6O2S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0247363
N-[5-[(3,5-dimethylmorpholin-4-yl)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H32N6O3S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0201612
(S)-N-(5-((3,3-dimethylbutan-2-ylamino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H34N6O2S
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0035803
N-[1-(2-hydroxy-2-methylpropyl)-5-[[methyl(pyridin-3-ylmethyl)amino]methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H29N7O2S
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0127792
N-[1-(2-hydroxy-2-methylpropyl)-5-(piperidin-1-ylmethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C25H30N6O2S
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0092569
N-[1-(2-hydroxy-2-methylpropyl)-5-[(2-methylpropylamino)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C24H30N6O2S
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0090966
N-[5-[[cyclohexyl(methyl)amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H34N6O2S
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0127793
N-[1-(2-hydroxy-2-methylpropyl)-5-(morpholin-4-ylmethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C24H28N6O3S
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0247359
N-[5-[(benzylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H28N6O2S
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0158361
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-formylthiophene-2-carboxamide
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C24H21N5O4S
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0092565
N-[5-[(cyclohexylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H32N6O2S
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0213273
N-[5-(anilinomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H26N6O2S
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0234405
N-[5-[(butan-2-ylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C24H30N6O2S
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0092566
N-[5-[(dimethylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C22H26N6O2S
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0279315
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyridin-3-yl)thiophene-2-carboxamide
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C28H24N6O3S
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0043198
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-oxazol-5-yl)thiophene-2-carboxamide
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C26H22N6O4S
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0218629
N-[5-[[2-(hydroxymethyl)piperidin-1-yl]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C26H32N6O3S
 1
1
IC50 = 58 nM
   TI
   LI
   LO
   TS
CP0043194
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C27H24N6O4S
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0178121
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-fluoropyridin-4-yl)thiophene-2-carboxamide
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C28H23FN6O3S
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0035798
N-[5-[[2-(dimethylamino)ethyl-methylamino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C25H33N7O2S
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0167147
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-cyanopyridin-4-yl)thiophene-2-carboxamide
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C29H23N7O3S
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0292211
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-3-phenylbenzamide
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C31H27N5O3
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0158363
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-oxazol-2-yl)thiophene-2-carboxamide
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C26H22N6O4S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0158365
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-bromothiophene-2-carboxamide
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C23H20BrN5O3S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0316933
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(5-cyanopyridin-3-yl)thiophene-2-carboxamide
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C29H23N7O3S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0035796
N-[5-[benzoyl(methyl)amino]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C28H27N5O4S
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0035802
N-[1-(2-hydroxy-2-methylpropyl)-5-[(N-methylanilino)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H28N6O2S
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0090963
N-[1-(2-hydroxy-2-methylpropyl)-5-[(3-hydroxypyrrolidin-1-yl)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C24H28N6O3S
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0043193
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-benzoylthiophene-2-carboxamide
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C30H25N5O4S
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0070415
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-5-cyanothiophene-2-carboxamide
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C24H20N6O3S
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0043135
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(ethyl)amino]benzimidazol-2-yl]-4-cyanobenzamide
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C27H24N6O3
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0090965
N-[5-(anilinomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C27H27N5O3S
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0090967
N-[5-[[cyclohexyl(methyl)amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C28H35N5O3S
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0070416
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-thiazol-2-yl)thiophene-2-carboxamide
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C26H22N6O3S2
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0152448
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(6-fluoropyridin-3-yl)thiophene-2-carboxamide
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C28H23FN6O3S
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0207058
N-[5-[(cyclohexylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C27H33N5O3S
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0555096
N-[1-(3-amino-3-oxopropyl)-5-[(4-chlorobenzoyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
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C26H21ClN6O3
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0316935
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(6-cyanopyridin-3-yl)thiophene-2-carboxamide
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C29H23N7O3S
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0776107
trans-5-(2-(1H-pyrazol-4-yl)vinyl)-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)thiophene-2-carboxamide
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C28H25N7O3S
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0127377
2-aminobenzimidazole with trans-stilbene, 9c
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C26H25N5O3S
 1
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
CP0739337
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1-cyanoprop-1-en-2-yl)thiophene-2-carboxamide
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C27H24N6O3S
 1
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
CP0170602
N-[1-(3-amino-3-oxopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]-4-cyanobenzamide
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C26H28N6O3
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0166422
N-[1-(3-amino-3-oxopropyl)-5-[(4-fluorobenzoyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
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C26H21FN6O3
 1
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0093047
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-4-cyanobenzamide
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C26H22N6O3
 2
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
2
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0093050
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-4-chlorobenzamide
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C25H22ClN5O3
 2
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
2
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0170594
N-[1-(3-amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]benzimidazol-5-yl]-N,4-dimethylbenzamide
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C27H24N6O3
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0310221
2-aminobenzimidazole with trans-stilbene, 8b
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C25H23N5O3S
 1
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0245732
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-acetylthiophene-2-carboxamide
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C25H23N5O4S
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0767300
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-cyanovinyl)thiophene-2-carboxamide
   Show/Hide
C26H22N6O3S
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0647648
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(5-aminopyrimidin-2-yl)vinyl)thiophene-2-carboxamide
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C29H26N8O3S
 1
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
CP0254690
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-phenoxythiophene-2-carboxamide
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C29H25N5O4S
 1
1
IC50 = 470 nM
   TI
   LI
   LO
   TS
CP0307538
N-[1-(3-amino-3-oxopropyl)-5-[methyl-[4-(trifluoromethoxy)benzoyl]amino]benzimidazol-2-yl]-4-cyanobenzamide
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C27H21F3N6O4
 1
1
IC50 = 500 nM
   TI
   LI
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   TS
CP0236293
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyridin-4-yl)thiophene-2-carboxamide
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C28H24N6O3S
 1
1
IC50 = 510 nM
   TI
   LI
   LO
   TS
CP0254695
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-chlorothiophene-2-carboxamide
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C23H20ClN5O3S
 1
1
IC50 = 520 nM
   TI
   LI
   LO
   TS
CP0043196
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]naphthalene-2-carboxamide
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C29H25N5O3
 1
1
IC50 = 540 nM
   TI
   LI
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   TS
CP0767280
trans-methyl 3-(5-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidenecarbamoyl)thiophen-2-yl)acrylate
   Show/Hide
C27H25N5O5S
 1
1
IC50 = 540 nM
   TI
   LI
   LO
   TS
CP0279314
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-methylpropanoyl)thiophene-2-carboxamide
   Show/Hide
C27H27N5O4S
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0039460
2-aminobenzimidazole with trans-stilbene, 8q
   Show/Hide
C31H28N6O3S
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0322865
2-aminobenzimidazole with trans-stilbene, 8f
   Show/Hide
C31H27N5O3S
 1
1
IC50 = 620 nM
   TI
   LI
   LO
   TS
CP0647651
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-aminostyryl)thiophene-2-carboxamide
   Show/Hide
C31H28N6O3S
 1
1
IC50 = 620 nM
   TI
   LI
   LO
   TS
CP0158362
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyridin-2-yl)thiophene-2-carboxamide
   Show/Hide
C28H24N6O3S
 1
1
IC50 = 650 nM
   TI
   LI
   LO
   TS
CP0647647
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyridin-3-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H26N6O3S
 1
1
IC50 = 690 nM
   TI
   LI
   LO
   TS
CP0235980
N-[1-(3-amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]benzimidazol-5-yl]-N-methylpyridine-3-carboxamide
   Show/Hide
C25H21N7O3
 1
1
IC50 = 720 nM
   TI
   LI
   LO
   TS
CP0036378
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyrazin-2-yl)thiophene-2-carboxamide
   Show/Hide
C27H23N7O3S
 1
1
IC50 = 730 nM
   TI
   LI
   LO
   TS
CP0279309
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-4-bromobenzamide
   Show/Hide
C25H22BrN5O3
 1
1
IC50 = 730 nM
   TI
   LI
   LO
   TS
CP0158364
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-oxazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H22N6O4S
 1
1
IC50 = 740 nM
   TI
   LI
   LO
   TS
CP0310222
2-aminobenzimidazole with trans-stilbene, 8s
   Show/Hide
C31H27N5O4S
 1
1
IC50 = 740 nM
   TI
   LI
   LO
   TS
CP0647645
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyridin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H26N6O3S
 1
1
IC50 = 760 nM
   TI
   LI
   LO
   TS
CP0647654
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyrazin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C29H25N7O3S
 1
1
IC50 = 810 nM
   TI
   LI
   LO
   TS
CP0334231
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-phenylthiophene-2-carboxamide
   Show/Hide
C29H25N5O3S
 1
1
IC50 = 820 nM
   TI
   LI
   LO
   TS
CP0739619
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1-(pyridin-4-yl)prop-1-en-2-yl)thiophene-2-carboxamide
   Show/Hide
C31H28N6O3S
 1
1
IC50 = 830 nM
   TI
   LI
   LO
   TS
CP0739333
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyridin-4-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H26N6O3S
 1
1
IC50 = 990 nM
   TI
   LI
   LO
   TS
CP0317417
N-[1-(3-amino-3-oxopropyl)-5-[(4-methoxybenzoyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C27H24N6O4
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0739620
trans-methyl 3-(5-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidenecarbamoyl)thiophen-2-yl)but-2-enoate
   Show/Hide
C28H27N5O5S
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0254698
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(benzyloxy)thiophene-2-carboxamide
   Show/Hide
C30H27N5O4S
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0186118
1-(3-amino-3-oxopropyl)-2-[(4-bromobenzoyl)amino]-N-cyclohexyl-N-prop-2-enylbenzimidazole-5-carboxamide
   Show/Hide
C27H30BrN5O3
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0252211
1-(3-amino-3-oxopropyl)-2-(4-bromobenzamido)-N-cyclohexyl-N-ethyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C26H30BrN5O3
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0349441
1-(3-amino-3-oxopropyl)-2-(4-bromobenzamido)-N-cyclohexyl-N-methyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H28BrN5O3
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0158290
5-(2-amino-1,3-thiazol-4-yl)-N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]thiophene-2-carboxamide
   Show/Hide
C26H23N7O3S2
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0647653
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(3-aminostyryl)thiophene-2-carboxamide
   Show/Hide
C31H28N6O3S
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0169839
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]thiophene-3-carboxamide
   Show/Hide
C23H21N5O3S
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0270244
N-cyclohexyl-N-methyl-1-propyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
   Show/Hide
C23H28N4O2S
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0767302
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1-(pyridin-3-yl)prop-1-en-2-yl)thiophene-2-carboxamide
   Show/Hide
C31H28N6O3S
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0437812
N-[1-(3-aminopropyl)-5-(cyclohexanecarbonylamino)benzimidazol-2-yl]thiophene-2-carboxamide
   Show/Hide
C22H27N5O2S
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0254694
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyrrolidin-1-yl)thiophene-2-carboxamide
   Show/Hide
C27H28N6O3S
 1
1
IC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0270243
N-cyclohexyl-N-methyl-1-(2-phenylethyl)-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
   Show/Hide
C28H30N4O2S
 1
1
IC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0310219
2-aminobenzimidazole with trans-stilbene, 8i
   Show/Hide
C32H29N5O4S
 1
1
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0203862
N-cyclohexyl-1-(3-hydroxypropyl)-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
   Show/Hide
C23H28N4O3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0647655
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(6-aminopyridin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H27N7O3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0257164
2-aminobenzimidazole with trans-stilbene, 8u
   Show/Hide
C28H25N7O3S
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0128130
N-[1-(3-amino-3-oxopropyl)-5-[(4,4-difluorocyclohexanecarbonyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C26H26F2N6O3
 1
1
IC50 = 2300 nM
   TI
   LI
   LO
   TS
CP0158359
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]benzamide
   Show/Hide
C25H23N5O3
 1
1
IC50 = 2300 nM
   TI
   LI
   LO
   TS
CP0020488
N-[1-(3-aminopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]thiophene-2-carboxamide
   Show/Hide
C23H29N5O2S
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0043191
BMCL186218 Compound 1
   Show/Hide
C23H21N5O3S
 2
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
2
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0217446
1-(3-amino-3-oxopropyl)-2-benzamido-N-methyl-N-phenyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H23N5O3
 1
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0103814
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(nicotinamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C24H28N6O3
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0104001
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C23H27N5O3S
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0039456
2-aminobenzimidazole with trans-stilbene, 9f
   Show/Hide
C32H29N5O3S
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0103811
1-(5-amino-5-oxopentyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H31N5O3S
 1
1
IC50 = 3100 nM
   TI
   LI
   LO
   TS
CP0202343
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(oxazole-5-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C22H26N6O4
 1
1
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0296100
1-(3-amino-3-oxopropyl)-N-cyclohexyl-2-(4-fluorobenzamido)-N-methyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H28FN5O3
 1
1
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0203865
1-(4-amino-4-oxobutyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C24H29N5O3S
 1
1
IC50 = 4600 nM
   TI
   LI
   LO
   TS
CP0217290
N-cyclohexyl-1-(2-hydroxyethyl)-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
   Show/Hide
C22H26N4O3S
 1
1
IC50 = 4600 nM
   TI
   LI
   LO
   TS
CP0253756
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(4-nitrobenzamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H28N6O5
 1
1
IC50 = 6900 nM
   TI
   LI
   LO
   TS
CP0340399
N-[1-(3-amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]benzimidazol-5-yl]-N-methylpyridine-4-carboxamide
   Show/Hide
C25H21N7O3
 1
1
IC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0270255
1-(3-amino-3-oxopropyl)-2-(4-cyanobenzamido)-N-cyclohexyl-N-methyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C26H28N6O3
 1
1
IC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0305900
1-(3-amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-prop-2-enylbenzimidazole-5-carboxamide
   Show/Hide
C27H31N5O3
 1
1
IC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0484967
1-(3-amino-3-oxopropyl)-N-cyclohexyl-2-(3-fluorobenzamido)-N-methyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H28FN5O3
 1
1
IC50 = 7400 nM
   TI
   LI
   LO
   TS
CP0339903
1-(3-amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-ethyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C26H31N5O3
 1
1
IC50 = 8100 nM
   TI
   LI
   LO
   TS
CP0253758
1-(3-amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-methyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C25H29N5O3
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0159905
N-[1-(3-aminopropyl)benzimidazol-2-yl]thiophene-2-carboxamide
   Show/Hide
C15H16N4OS
 1
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
CP0270256
1-(3-amino-3-oxopropyl)-N-cyclohexyl-2-(4-methoxybenzamido)-N-methyl-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C26H31N5O4
 1
1
IC50 = 17000 nM
   TI
   LI
   LO
   TS
CP0174286
1-(3-aminopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C23H29N5O2S
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0276426
3-(3-aminopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-3H-benzo[d]imidazole-5-carboxamide
   Show/Hide
C23H29N5O2S
 1
1
IC50 = 20000 nM
   TI
   LI
   LO
   TS
CP0174288
N-cyclohexyl-N-methyl-1-[3-(methylamino)-3-oxopropyl]-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
   Show/Hide
C24H29N5O3S
 1
1
IC50 = 24000 nM
   TI
   LI
   LO
   TS
CP0043195
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(morpholin-4-yl)thiophene-2-carboxamide
   Show/Hide
C27H28N6O4S
 1
1
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0043200
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(piperidin-1-yl)thiophene-2-carboxamide
   Show/Hide
C28H30N6O3S
 1
1
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0279310
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(piperazin-1-yl)thiophene-2-carboxamide
   Show/Hide
C27H29N7O3S
 1
1
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0043190
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-4-phenylbenzamide
   Show/Hide
C31H27N5O3
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0043197
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-thiazole-5-carboxamide
   Show/Hide
C22H20N6O3S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0236292
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-4-methoxybenzamide
   Show/Hide
C26H25N5O4
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0279312
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]naphthalene-1-carboxamide
   Show/Hide
C29H25N5O3
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0279313
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-oxazole-4-carboxamide
   Show/Hide
C22H20N6O4
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0292212
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-thiazole-4-carboxamide
   Show/Hide
C22H20N6O3S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0305251
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-oxazole-2-carboxamide
   Show/Hide
C22H20N6O4
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0316931
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-1,2-oxazole-5-carboxamide
   Show/Hide
C22H20N6O4
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0318793
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-oxazole-5-carboxamide
   Show/Hide
C22H20N6O4
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0039455
2-aminobenzimidazole with trans-stilbene, 8m
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C32H26F3N5O3S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0212266
2-aminobenzimidazole with trans-stilbene, 8h
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C32H29N5O4S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0212267
2-aminobenzimidazole with trans-stilbene, 8l
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C32H26F3N5O3S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0219965
2-aminobenzimidazole with trans-stilbene, 8k
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C32H26F3N5O3S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0310574
2-aminobenzimidazole with trans-stilbene, 8j
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C32H29N5O4S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0739618
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(3-nitrostyryl)thiophene-2-carboxamide
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C31H26N6O5S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0035800
N-[1-(2-hydroxy-2-methylpropyl)-5-[(N-methylanilino)methyl]benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
   Show/Hide
C28H29N5O3S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0127794
N-[5-(aminomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C20H22N6O2S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0207056
N-[1-(2-hydroxy-2-methylpropyl)-5-(methylaminomethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C21H24N6O2S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0035801
(S)-N-(5-(((3,3-dimethylbutan-2-yl)(methyl)amino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C27H36N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 8 nM
CP0035803
N-[1-(2-hydroxy-2-methylpropyl)-5-[[methyl(pyridin-3-ylmethyl)amino]methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C27H29N7O2S
 2
1 IC50 = 1 nM
2 IC50 = 100 nM
CP0035804
(R)-N-(5-(((3,3-dimethylbutan-2-yl)(methyl)amino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C27H36N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 20 nM
CP0071438
(R)-N-(5-((3,3-dimethylbutan-2-ylamino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H34N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 20 nM
CP0092565
N-[5-[(cyclohexylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H32N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 99 nM
CP0092569
N-[1-(2-hydroxy-2-methylpropyl)-5-[(2-methylpropylamino)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C24H30N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 140 nM
CP0201612
(S)-N-(5-((3,3-dimethylbutan-2-ylamino)methyl)-1-(2-hydroxy-2-methylpropyl)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H34N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 13 nM
CP0247359
N-[5-[(benzylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C27H28N6O2S
 2
1 IC50 = 1 nM
2 IC50 = 140 nM
CP0247363
N-[5-[(3,5-dimethylmorpholin-4-yl)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H32N6O3S
 2
1 IC50 = 1 nM
2 IC50 = 98 nM
CP0166422
N-[1-(3-amino-3-oxopropyl)-5-[(4-fluorobenzoyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C26H21FN6O3
 1
1 IC50 = 2 nM
CP0043198
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-oxazol-5-yl)thiophene-2-carboxamide
   Show/Hide
C26H22N6O4S
 1
1 IC50 = 2 nM
CP0043199
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H23N7O3S
 1
1 IC50 = 2 nM
CP0158361
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-formylthiophene-2-carboxamide
   Show/Hide
C24H21N5O4S
 1
1 IC50 = 2 nM
CP0236293
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyridin-4-yl)thiophene-2-carboxamide
   Show/Hide
C28H24N6O3S
 1
1 IC50 = 2 nM
CP0316933
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(5-cyanopyridin-3-yl)thiophene-2-carboxamide
   Show/Hide
C29H23N7O3S
 1
1 IC50 = 2 nM
CP0035798
N-[5-[[2-(dimethylamino)ethyl-methylamino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C25H33N7O2S
 2
1 IC50 = 2 nM
2 IC50 = 180 nM
CP0090963
N-[1-(2-hydroxy-2-methylpropyl)-5-[(3-hydroxypyrrolidin-1-yl)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C24H28N6O3S
 2
1 IC50 = 2 nM
2 IC50 = 310 nM
CP0090966
N-[5-[[cyclohexyl(methyl)amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C27H34N6O2S
 2
1 IC50 = 2 nM
2 IC50 = 160 nM
CP0127793
N-[1-(2-hydroxy-2-methylpropyl)-5-(morpholin-4-ylmethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C24H28N6O3S
 2
1 IC50 = 2 nM
2 IC50 = 220 nM
CP0207056
N-[1-(2-hydroxy-2-methylpropyl)-5-(methylaminomethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C21H24N6O2S
 2
1 IC50 = 2 nM
2 IC50 = 420 nM
CP0213273
N-[5-(anilinomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H26N6O2S
 2
1 IC50 = 2 nM
2 IC50 = 75 nM
CP0234405
N-[5-[(butan-2-ylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C24H30N6O2S
 2
1 IC50 = 2 nM
2 IC50 = 390 nM
CP0193276
3-[4-amino-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(3-methyl-4-propan-2-ylphenyl)benzamide
   Show/Hide
C30H33N7O2
 2
1 IC50 = 2 nM
2 IC50 = 48 nM
CP0007430
IBRUTINIB
   Show/Hide
C25H24N6O2
 9
1 IC50 = 2.7 nM
2 IC50 = 3 nM
3 IC50 = 4.9 nM
4 IC50 = 10.7 nM
5 IC50 = 13.9 nM
6 IC50 = 33.7 nM
7 IC50 = 99 nM
8 Kd = 57 nM
9 Kd = 63 nM
CP0093047
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C26H22N6O3
 4
1 IC50 = 3 nM
2 IC50 = 12 nM
3 IC50 = 17 nM
4 IC50 = 20 nM
CP0158359
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]benzamide
   Show/Hide
C25H23N5O3
 2
1 IC50 = 3 nM
2 IC50 = 180 nM
CP0178121
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-fluoropyridin-4-yl)thiophene-2-carboxamide
   Show/Hide
C28H23FN6O3S
 1
1 IC50 = 3 nM
CP0035796
N-[5-[benzoyl(methyl)amino]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
   Show/Hide
C28H27N5O4S
 2
1 IC50 = 3 nM
2 IC50 = 200 nM
CP0092566
N-[5-[(dimethylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C22H26N6O2S
 2
1 IC50 = 3 nM
2 IC50 = 490 nM
CP0127792
N-[1-(2-hydroxy-2-methylpropyl)-5-(piperidin-1-ylmethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C25H30N6O2S
 2
1 IC50 = 3 nM
2 IC50 = 250 nM
CP0218629
N-[5-[[2-(hydroxymethyl)piperidin-1-yl]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C26H32N6O3S
 2
1 IC50 = 3 nM
2 IC50 = 660 nM
CP0165797
US9573958, Compound 59
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C28H35F2N5O2S
 1
1 IC50 = 3.2 nM
CP0170602
N-[1-(3-amino-3-oxopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C26H28N6O3
 1
1 IC50 = 4 nM
CP0235980
N-[1-(3-amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]benzimidazol-5-yl]-N-methylpyridine-3-carboxamide
   Show/Hide
C25H21N7O3
 1
1 IC50 = 4 nM
CP0253827
N-[1-(3-amino-3-oxopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]-4-chlorobenzamide
   Show/Hide
C25H28ClN5O3
 1
1 IC50 = 4 nM
CP0307187
4-cyano-N-[5-[cyclohexanecarbonyl(methyl)amino]-1-(3-imidazol-1-ylpropyl)benzimidazol-2-yl]benzamide
   Show/Hide
C29H31N7O2
 1
1 IC50 = 4 nM
CP0127794
N-[5-(aminomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
   Show/Hide
C20H22N6O2S
 2
1 IC50 = 4 nM
2 IC50 = 900 nM
CP0013795
N-[2-[[6-benzyl-2-[6-(difluoromethyl)-1H-indazol-3-yl]-1H-indol-4-yl]oxy]ethyl]prop-2-enamide
   Show/Hide
C28H24F2N4O2
 2
1 IC50 = 4 nM
2 Ki = 13 nM
CP0152448
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(6-fluoropyridin-3-yl)thiophene-2-carboxamide
   Show/Hide
C28H23FN6O3S
 1
1 IC50 = 5 nM
CP0279315
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyridin-3-yl)thiophene-2-carboxamide
   Show/Hide
C28H24N6O3S
 1
1 IC50 = 5 nM
CP0647647
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyridin-3-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H26N6O3S
 1
1 IC50 = 5 nM
CP0647648
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(5-aminopyrimidin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C29H26N8O3S
 1
1 IC50 = 5 nM
CP0767300
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-cyanovinyl)thiophene-2-carboxamide
   Show/Hide
C26H22N6O3S
 1
1 IC50 = 5 nM
CP0086763
N-[2-[[6-benzyl-2-[6-(1H-pyrazol-4-yl)-1H-indazol-3-yl]-1H-indol-4-yl]oxy]ethyl]prop-2-enamide
   Show/Hide
C30H26N6O2
 2
1 IC50 = 5.8 nM
2 Ki = 20 nM
CP0093050
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-4-chlorobenzamide
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C25H22ClN5O3
 2
1 IC50 = 6 nM
2 IC50 = 18 nM
CP0043194
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
   Show/Hide
C27H24N6O4S
 1
1 IC50 = 6 nM
CP0039460
2-aminobenzimidazole with trans-stilbene, 8q
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C31H28N6O3S
 1
1 IC50 = 6 nM
CP0647645
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyridin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H26N6O3S
 1
1 IC50 = 6 nM
CP0647651
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-aminostyryl)thiophene-2-carboxamide
   Show/Hide
C31H28N6O3S
 1
1 IC50 = 6 nM
CP0043135
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(ethyl)amino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C27H24N6O3
 1
1 IC50 = 7 nM
CP0317417
N-[1-(3-amino-3-oxopropyl)-5-[(4-methoxybenzoyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
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C27H24N6O4
 1
1 IC50 = 7 nM
CP0310221
2-aminobenzimidazole with trans-stilbene, 8b
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C25H23N5O3S
 1
1 IC50 = 7 nM
CP0647655
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(6-aminopyridin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C30H27N7O3S
 1
1 IC50 = 7 nM
CP0070415
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-5-cyanothiophene-2-carboxamide
   Show/Hide
C24H20N6O3S
 2
1 IC50 = 8 nM
2 IC50 = 15 nM
CP0128130
N-[1-(3-amino-3-oxopropyl)-5-[(4,4-difluorocyclohexanecarbonyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
   Show/Hide
C26H26F2N6O3
 1
1 IC50 = 8 nM
CP0158363
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-oxazol-2-yl)thiophene-2-carboxamide
   Show/Hide
C26H22N6O4S
 1
1 IC50 = 8 nM
CP0167147
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-cyanopyridin-4-yl)thiophene-2-carboxamide
   Show/Hide
C29H23N7O3S
 1
1 IC50 = 8 nM
CP0647654
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyrazin-2-yl)vinyl)thiophene-2-carboxamide
   Show/Hide
C29H25N7O3S
 1
1 IC50 = 8 nM
CP0035802
N-[1-(2-hydroxy-2-methylpropyl)-5-[(N-methylanilino)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamide
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C27H28N6O2S
 2
1 IC50 = 8 nM
2 IC50 = 780 nM
CP0090967
N-[5-[[cyclohexyl(methyl)amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
   Show/Hide
C28H35N5O3S
 2
1 IC50 = 8 nM
2 IC50 = 670 nM
CP0207058
N-[5-[(cyclohexylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
   Show/Hide
C27H33N5O3S
 2
1 IC50 = 8 nM
2 IC50 = 940 nM
CP0310222
2-aminobenzimidazole with trans-stilbene, 8s
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C31H27N5O4S
 1
1 IC50 = 9 nM
CP0647653
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(3-aminostyryl)thiophene-2-carboxamide
   Show/Hide
C31H28N6O3S
 1
1 IC50 = 9 nM
CP0776107
trans-5-(2-(1H-pyrazol-4-yl)vinyl)-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)thiophene-2-carboxamide
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C28H25N7O3S
 1
1 IC50 = 9 nM
CP0170594
N-[1-(3-amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]benzimidazol-5-yl]-N,4-dimethylbenzamide
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C27H24N6O3
 1
1 IC50 = 10 nM
CP0316931
N-[1-(3-amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-1,2-oxazole-5-carboxamide
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C22H20N6O4
 2
1 IC50 = 10 nM
2 IC50 = 100 nM
CP0158290
5-(2-amino-1,3-thiazol-4-yl)-N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]thiophene-2-carboxamide
   Show/Hide
C26H23N7O3S2
 1
1 IC50 = 10 nM
CP0316935
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(6-cyanopyridin-3-yl)thiophene-2-carboxamide
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C29H23N7O3S
 1
1 IC50 = 10 nM
CP0767280
trans-methyl 3-(5-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidenecarbamoyl)thiophen-2-yl)acrylate
   Show/Hide
C27H25N5O5S
 1
1 IC50 = 10 nM
CP0188023
3-[4-amino-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-propan-2-ylphenyl)benzamide
   Show/Hide
C29H31N7O2
 2
1 IC50 = 10 nM
2 IC50 = 40 nM
CP0188026
3-[4-amino-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-[(4-tert-butylphenyl)methyl]benzamide
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C31H35N7O2
 2
1 IC50 = 10 nM
2 IC50 = 6731 nM
CP0266648
3-[4-amino-1-[(3R)-1-prop-2-ynoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-propan-2-ylphenyl)benzamide
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C29H29N7O2
 1
1 IC50 = 10 nM
CP0247677
3-[4-amino-1-(1-prop-2-enoylpiperidin-3-yl)pyrazolo[3,4-d]pyrimidin-3-yl]-N-(3-tert-butylphenyl)benzamide
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C30H33N7O2
 2
1 IC50 = 10 nM
2 IC50 = 73 nM
CP0070416
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-thiazol-2-yl)thiophene-2-carboxamide
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C26H22N6O3S2
 1
1 IC50 = 11 nM
CP0322865
2-aminobenzimidazole with trans-stilbene, 8f
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C31H27N5O3S
 1
1 IC50 = 11 nM
CP0090965
N-[5-(anilinomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C27H27N5O3S
 2
1 IC50 = 11 nM
2 IC50 > 5000 nM
CP0088490
US10894048, Ref. Ex Comp. 1
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C25H24N6O2
 1
1 IC50 = 11 nM
CP0555096
N-[1-(3-amino-3-oxopropyl)-5-[(4-chlorobenzoyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamide
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C26H21ClN6O3
 1
1 IC50 = 12 nM
CP0257164
2-aminobenzimidazole with trans-stilbene, 8u
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C28H25N7O3S
 1
1 IC50 = 12 nM
CP0036378
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyrazin-2-yl)thiophene-2-carboxamide
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C27H23N7O3S
 1
1 IC50 = 13 nM
CP0310219
2-aminobenzimidazole with trans-stilbene, 8i
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C32H29N5O4S
 1
1 IC50 = 13 nM
CP0043191
BMCL186218 Compound 1
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C23H21N5O3S
 3
1 IC50 = 14 nM
2 IC50 = 25 nM
3 IC50 = 58 nM
CP0158364
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(1,3-oxazol-4-yl)thiophene-2-carboxamide
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C26H22N6O4S
 1
1 IC50 = 14 nM
CP0245732
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-acetylthiophene-2-carboxamide
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C25H23N5O4S
 1
1 IC50 = 14 nM
CP0254695
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-chlorothiophene-2-carboxamide
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C23H20ClN5O3S
 1
1 IC50 = 14 nM
CP0158365
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-bromothiophene-2-carboxamide
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C23H20BrN5O3S
 1
1 IC50 = 15 nM
CP0158362
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyridin-2-yl)thiophene-2-carboxamide
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C28H24N6O3S
 1
1 IC50 = 19 nM
CP0279314
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(2-methylpropanoyl)thiophene-2-carboxamide
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C27H27N5O4S
 1
1 IC50 = 20 nM
CP0020488
N-[1-(3-aminopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]thiophene-2-carboxamide
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C23H29N5O2S
 5
1 IC50 = 25 nM
2 IC50 = 110 nM
3 IC50 = 320 nM
4 IC50 = 1600 nM
5 IC50 > 5000 nM
CP0279309
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-4-bromobenzamide
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C25H22BrN5O3
 1
1 IC50 = 26 nM
CP0340399
N-[1-(3-amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]benzimidazol-5-yl]-N-methylpyridine-4-carboxamide
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C25H21N7O3
 1
1 IC50 = 27 nM
CP0212267
2-aminobenzimidazole with trans-stilbene, 8l
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C32H26F3N5O3S
 1
1 IC50 = 30 nM
CP0307538
N-[1-(3-amino-3-oxopropyl)-5-[methyl-[4-(trifluoromethoxy)benzoyl]amino]benzimidazol-2-yl]-4-cyanobenzamide
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C27H21F3N6O4
 1
1 IC50 = 35 nM
CP0254698
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(benzyloxy)thiophene-2-carboxamide
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C30H27N5O4S
 1
1 IC50 = 35 nM
CP0075453
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-5-[(3,3-dimethylbutan-2-ylamino)methyl]-1H-pyrrole-2-carboxamide
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C31H42N6O3S2
 1
1 IC50 = 35 nM
CP0127377
2-aminobenzimidazole with trans-stilbene, 9c
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C26H25N5O3S
 1
1 IC50 = 37 nM
CP0334231
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-phenylthiophene-2-carboxamide
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C29H25N5O3S
 1
1 IC50 = 39 nM
CP0739620
trans-methyl 3-(5-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidenecarbamoyl)thiophen-2-yl)but-2-enoate
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C28H27N5O5S
 1
1 IC50 = 39 nM
CP0767302
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1-(pyridin-3-yl)prop-1-en-2-yl)thiophene-2-carboxamide
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C31H28N6O3S
 1
1 IC50 = 39 nM
CP0156889
N-[1-(3-amino-3-oxopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]thiophene-2-carboxamide
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C23H27N5O3S
 1
1 IC50 = 40 nM
CP0075454
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-piperazin-1-ylbenzamide
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C30H36N6O3S2
 1
1 IC50 = 40 nM
CP0739618
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(3-nitrostyryl)thiophene-2-carboxamide
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C31H26N6O5S
 1
1 IC50 = 42 nM
CP0060760
US9447106, 27b (peak 2)
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C27H29N5O3
 4
1 IC50 = 50 nM
2 IC50 = 56 nM
3 IC50 = 3477 nM
4 Kd = 30000 nM
CP0043193
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-benzoylthiophene-2-carboxamide
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C30H25N5O4S
 1
1 IC50 = 55 nM
CP0169839
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]thiophene-3-carboxamide
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C23H21N5O3S
 1
1 IC50 = 57 nM
CP0310574
2-aminobenzimidazole with trans-stilbene, 8j
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C32H29N5O4S
 1
1 IC50 = 58 nM
CP0739619
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1-(pyridin-4-yl)prop-1-en-2-yl)thiophene-2-carboxamide
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C31H28N6O3S
 1
1 IC50 = 59 nM
CP0103811
1-(5-amino-5-oxopentyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
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C25H31N5O3S
 1
1 IC50 = 60 nM
CP0202343
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(oxazole-5-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
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C22H26N6O4
 1
1 IC50 = 62 nM
CP0739337
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(1-cyanoprop-1-en-2-yl)thiophene-2-carboxamide
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C27H24N6O3S
 1
1 IC50 = 63 nM
CP0739333
trans-N-(1-(3-amino-3-oxopropyl)-5-(N-methylbenzamido)-1H-benzo[d]imidazol-2(3H)-ylidene)-5-(2-(pyridin-4-yl)vinyl)thiophene-2-carboxamide
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C30H26N6O3S
 1
1 IC50 = 65 nM
CP0212266
2-aminobenzimidazole with trans-stilbene, 8h
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C32H29N5O4S
 1
1 IC50 = 67 nM
CP0103814
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(nicotinamido)-1H-benzo[d]imidazole-5-carboxamide
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C24H28N6O3
 1
1 IC50 = 69 nM
CP0043195
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(morpholin-4-yl)thiophene-2-carboxamide
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C27H28N6O4S
 1
1 IC50 = 74 nM
CP0039456
2-aminobenzimidazole with trans-stilbene, 9f
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C32H29N5O3S
 1
1 IC50 = 75 nM
CP0253756
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(4-nitrobenzamido)-1H-benzo[d]imidazole-5-carboxamide
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C25H28N6O5
 1
1 IC50 = 76 nM
CP0254694
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(pyrrolidin-1-yl)thiophene-2-carboxamide
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C27H28N6O3S
 1
1 IC50 = 81 nM
CP0252211
1-(3-amino-3-oxopropyl)-2-(4-bromobenzamido)-N-cyclohexyl-N-ethyl-1H-benzo[d]imidazole-5-carboxamide
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C26H30BrN5O3
 1
1 IC50 = 81 nM
CP0140867
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide
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C33H43N5O3S2
 2
1 IC50 = 90 nM
2 IC50 = 96 nM
CP0203862
N-cyclohexyl-1-(3-hydroxypropyl)-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
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C23H28N4O3S
 1
1 IC50 = 92 nM
CP0043196
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]naphthalene-2-carboxamide
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C29H25N5O3
 1
1 IC50 = 95 nM
CP0109389
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-[[(1-hydroxy-3-methylbutan-2-yl)amino]methyl]benzamide
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C32H41N5O4S2
 1
1 IC50 = 96 nM
CP0035800
N-[1-(2-hydroxy-2-methylpropyl)-5-[(N-methylanilino)methyl]benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamide
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C28H29N5O3S
 2
1 IC50 = 100 nM
2 IC50 > 5000 nM
CP0194959
3-[4-amino-1-[(3R)-1-[(E)-4-[4-(2-aminoethyl)piperazin-1-yl]but-2-enoyl]piperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-propan-2-ylphenyl)benzamide
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C36H46N10O2
 1
1 IC50 = 100 nM
CP0104001
1-(3-amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
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C23H27N5O3S
 1
1 IC50 = 110 nM
CP0484967
1-(3-amino-3-oxopropyl)-N-cyclohexyl-2-(3-fluorobenzamido)-N-methyl-1H-benzo[d]imidazole-5-carboxamide
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C25H28FN5O3
 1
1 IC50 = 110 nM
CP0043197
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-thiazole-5-carboxamide
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C22H20N6O3S
 1
1 IC50 = 130 nM
CP0039455
2-aminobenzimidazole with trans-stilbene, 8m
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C32H26F3N5O3S
 1
1 IC50 = 130 nM
CP0254690
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-phenoxythiophene-2-carboxamide
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C29H25N5O4S
 1
1 IC50 = 140 nM
CP0333453
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-1H-pyrrole-2-carboxamide
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C24H27N5O3S2
 1
1 IC50 = 140 nM
CP0203865
1-(4-amino-4-oxobutyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
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C24H29N5O3S
 1
1 IC50 = 140 nM
CP0279310
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(piperazin-1-yl)thiophene-2-carboxamide
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C27H29N7O3S
 1
1 IC50 = 150 nM
CP0174288
N-cyclohexyl-N-methyl-1-[3-(methylamino)-3-oxopropyl]-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
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C24H29N5O3S
 1
1 IC50 = 160 nM
CP0236292
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-4-methoxybenzamide
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C26H25N5O4
 1
1 IC50 = 170 nM
CP0279313
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-oxazole-4-carboxamide
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C22H20N6O4
 1
1 IC50 = 170 nM
CP0318793
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-oxazole-5-carboxamide
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C22H20N6O4
 1
1 IC50 = 180 nM
CP0217290
N-cyclohexyl-1-(2-hydroxyethyl)-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
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C22H26N4O3S
 1
1 IC50 = 190 nM
CP0270255
1-(3-amino-3-oxopropyl)-2-(4-cyanobenzamido)-N-cyclohexyl-N-methyl-1H-benzo[d]imidazole-5-carboxamide
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C26H28N6O3
 1
1 IC50 = 200 nM
CP0186118
1-(3-amino-3-oxopropyl)-2-[(4-bromobenzoyl)amino]-N-cyclohexyl-N-prop-2-enylbenzimidazole-5-carboxamide
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C27H30BrN5O3
 1
1 IC50 = 230 nM
CP0296100
1-(3-amino-3-oxopropyl)-N-cyclohexyl-2-(4-fluorobenzamido)-N-methyl-1H-benzo[d]imidazole-5-carboxamide
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C25H28FN5O3
 1
1 IC50 = 250 nM
CP0349441
1-(3-amino-3-oxopropyl)-2-(4-bromobenzamido)-N-cyclohexyl-N-methyl-1H-benzo[d]imidazole-5-carboxamide
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C25H28BrN5O3
 1
1 IC50 = 260 nM
CP0219965
2-aminobenzimidazole with trans-stilbene, 8k
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C32H26F3N5O3S
 1
1 IC50 = 270 nM
CP0154955
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-(dimethylamino)benzamide
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C28H33N5O3S2
 1
1 IC50 = 300 nM
CP0159383
N-[5-[[3-(4-acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-(hydroxymethyl)benzamide
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C27H30N4O4S2
 1
1 IC50 = 320 nM
CP0217446
1-(3-amino-3-oxopropyl)-2-benzamido-N-methyl-N-phenyl-1H-benzo[d]imidazole-5-carboxamide
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C25H23N5O3
 1
1 IC50 = 330 nM
CP0292212
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-thiazole-4-carboxamide
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C22H20N6O3S
 1
1 IC50 = 340 nM
CP0253758
1-(3-amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-methyl-1H-benzo[d]imidazole-5-carboxamide
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C25H29N5O3
 1
1 IC50 = 370 nM
CP0043200
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-5-(piperidin-1-yl)thiophene-2-carboxamide
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C28H30N6O3S
 1
1 IC50 = 380 nM
CP0339903
1-(3-amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-ethyl-1H-benzo[d]imidazole-5-carboxamide
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C26H31N5O3
 1
1 IC50 = 390 nM
CP0266645
3-[4-amino-1-[(3S)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-propan-2-ylphenyl)benzamide
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C29H31N7O2
 2
1 IC50 = 400 nM
2 IC50 = 780 nM
CP0305251
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-1,3-oxazole-2-carboxamide
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C22H20N6O4
 1
1 IC50 = 450 nM
CP0276426
3-(3-aminopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-3H-benzo[d]imidazole-5-carboxamide
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C23H29N5O2S
 1
1 IC50 = 710 nM
CP0305900
1-(3-amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-prop-2-enylbenzimidazole-5-carboxamide
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C27H31N5O3
 1
1 IC50 = 730 nM
CP0270244
N-cyclohexyl-N-methyl-1-propyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
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C23H28N4O2S
 1
1 IC50 = 760 nM
CP0174286
1-(3-aminopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carboxamido)-1H-benzo[d]imidazole-5-carboxamide
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C23H29N5O2S
 1
1 IC50 = 950 nM
CP0292211
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-3-phenylbenzamide
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C31H27N5O3
 1
1 IC50 = 1000 nM
CP0270256
1-(3-amino-3-oxopropyl)-N-cyclohexyl-2-(4-methoxybenzamido)-N-methyl-1H-benzo[d]imidazole-5-carboxamide
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C26H31N5O4
 1
1 IC50 = 1100 nM
CP0270243
N-cyclohexyl-N-methyl-1-(2-phenylethyl)-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamide
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C28H30N4O2S
 1
1 IC50 = 1300 nM
CP0159905
N-[1-(3-aminopropyl)benzimidazol-2-yl]thiophene-2-carboxamide
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C15H16N4OS
 1
1 IC50 = 1500 nM
CP0279312
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]naphthalene-1-carboxamide
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C29H25N5O3
 1
1 IC50 = 2500 nM
CP0437812
N-[1-(3-aminopropyl)-5-(cyclohexanecarbonylamino)benzimidazol-2-yl]thiophene-2-carboxamide
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C22H27N5O2S
 1
1 IC50 = 2500 nM
CP0043190
N-[(2E)-5-[benzene(methyl)amido]-1-(2-carbamoylethyl)-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene]-4-phenylbenzamide
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C31H27N5O3
 1
1 IC50 = 10000 nM
CP0534851
N-[3-[6-cyclohexyl-2-[3-(2-methoxyethoxy)anilino]-7-oxopteridin-8-yl]phenyl]prop-2-enamide
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C30H32N6O4
 1
1 IC50 > 1000 nM
CP0086121
ACP-196
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C26H23N7O2
 4
1 IC50 > 1000 nM
2 IC50 > 10000 nM
3 Kd = 12000 nM
4 Kd > 10000 nM
CP0674816
(4aS,5aR)-N-[1-[(R)-[(2R)-1,1-dioxothian-2-yl]-phenyl-methyl]pyrazol-4-yl]-5,5-difluoro-5a-methyl-1,4,4a,6-tetrahydrocyclopropa[f]indazole-3-carboxamide
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C25H27F2N5O3S
 1
1 Ki = 0.09 nM
CP0488503
N-[1-[(1S)-3-(dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6-(1H-pyrazol-4-yl)-1H-indazole-3-carboxamide
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C25H26N8O
 1
1 Ki = 0.1 nM
CP0410454
6,6-dimethyl-N-[1-[(S)-phenyl(piperidin-4-yl)methyl]pyrazol-4-yl]-1,4,5,7-tetrahydroindazole-3-carboxamide
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C25H32N6O
 1
1 Ki = 0.2 nM
CP0953346
(4aS,5aR)-N-[1-[(S)-(1,1-dioxothian-4-yl)-phenyl-methyl]pyrazol-4-yl]-5a-methyl-4,4a,5,6-tetrahydro-1H-cyclopropa[f]indazole-3-carboxamide
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C25H29N5O3S
 1
1 Ki = 0.2 nM
CP0076932
N-[1-[(1R)-2-hydroxy-2-methyl-1-phenylpropyl]pyrazol-4-yl]-6-(1H-pyrazol-4-yl)-1H-indazole-3-carboxamide
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C24H23N7O2
 1
1 Ki = 0.23 nM
CP0282317
N-[1-[(S)-(1,1-dioxothian-4-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C25H31N5O3S
 1
1 Ki = 0.3 nM
CP0256792
(1S,2S)-2-[3-(diethylaminomethyl)-4-methoxyphenyl]-N-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C26H29N5O2S
 1
1 Ki = 0.5 nM
CP0051649
6,6-dimethyl-N-[1-[(1R)-2-methylsulfonyl-1-phenylethyl]pyrazol-4-yl]-1,4,5,7-tetrahydroindazole-3-carboxamide
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C22H27N5O3S
 1
1 Ki = 0.5 nM
CP0339362
2-[4-[(dimethylamino)methyl]phenyl]-N-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C23H23N5OS
 1
1 Ki = 0.6 nM
CP0176435
(1S,2S)-2-[4-[(dimethylamino)methyl]phenyl]-N-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C23H23N5OS
 1
1 Ki = 0.7 nM
CP0051651
N-[1-[(1S)-3-(dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C24H32N6O
 1
1 Ki = 0.7 nM
CP0116087
N-[1-[(1S)-3-(dimethylamino)-1-(3-methylphenyl)propyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C25H34N6O
 1
1 Ki = 0.7 nM
CP0122694
N-[1-[(3-cyanophenyl)methyl]pyrazol-4-yl]-6-(1H-pyrazol-4-yl)-1H-indazole-3-carboxamide
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C22H16N8O
 2
1 Ki = 0.8 nM
2 Ki = 1.1 nM
CP0476043
N-[1-[(1R)-2-(dimethylamino)-1-phenylethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C23H30N6O
 1
1 Ki = 0.8 nM
CP0057514
N-[1-[(1S)-1-(3-chlorophenyl)-3-(dimethylamino)propyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C24H31ClN6O
 1
1 Ki = 1.2 nM
CP0308473
(1S,2S)-2-[3-[(dimethylamino)methyl]phenyl]-N-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C23H23N5OS
 1
1 Ki = 1.9 nM
CP0270728
(1S,2S)-2-(4-methoxyphenyl)-N-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C21H18N4O2S
 1
1 Ki = 2.5 nM
CP0155504
(1S,2S)-N-[6-[5-(hydroxymethyl)pyridin-3-yl]-1,3-benzothiazol-2-yl]-2-(4-methoxyphenyl)cyclopropane-1-carboxamide
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C24H21N3O3S
 1
1 Ki = 5.3 nM
CP0258696
N-(1-benzylpyrazol-4-yl)-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C20H23N5O
 1
1 Ki = 5.3 nM
CP0271711
6,6-dimethyl-N-[1-[(1S)-3-methylsulfonyl-1-phenylpropyl]pyrazol-4-yl]-1,4,5,7-tetrahydroindazole-3-carboxamide
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C23H29N5O3S
 1
1 Ki = 6.2 nM
CP0286440
2-(4-methoxyphenyl)-N-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C21H18N4O2S
 1
1 Ki = 6.4 nM
CP0296084
(1S,2S)-2-(4-methoxyphenyl)-N-[6-(2-oxo-1H-pyridin-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C23H19N3O3S
 1
1 Ki = 6.6 nM
CP0334261
(1S,2S)-2-[4-[(dimethylamino)methyl]phenyl]-N-(6-pyridin-3-yl-1,3-benzothiazol-2-yl)cyclopropane-1-carboxamide
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C25H24N4OS
 1
1 Ki = 8.4 nM
CP0057512
N-(1-benzylpyrazol-4-yl)spiro[1,4,5,7-tetrahydroindazole-6,1'-cyclopropane]-3-carboxamide
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C20H21N5O
 1
1 Ki = 10 nM
CP0229652
N-[1-[(3-cyanophenyl)methyl]pyrazol-4-yl]-1H-indazole-3-carboxamide
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C19H14N6O
 2
1 Ki = 15 nM
2 Ki = 43 nM
CP0245646
N-[1-[(1R)-3-(dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide
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C24H32N6O
 1
1 Ki = 15 nM
CP0334263
(1S,2S)-2-(4-methoxyphenyl)-N-[6-(5-methyl-1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C22H20N4O2S
 1
1 Ki = 30 nM
CP0256793
(1S,2S)-2-(4-methoxyphenyl)-N-[6-(1-methylpyrazol-4-yl)-1,3-benzothiazol-2-yl]cyclopropane-1-carboxamide
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C22H20N4O2S
 1
1 Ki = 43 nM
CP0368731
(1S,2S)-2-phenyl-N-(6-pyridin-4-yl-1,3-benzothiazol-2-yl)cyclopropane-1-carboxamide
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C22H17N3OS
 1
1 Ki = 50 nM
CP0308475
(1S,2S)-2-phenyl-N-(6-pyridin-3-yl-1,3-benzothiazol-2-yl)cyclopropane-1-carboxamide
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C22H17N3OS
 1
1 Ki = 85 nM
CP0340468
(1S,2S)-2-phenyl-N-(6-pyridin-2-yl-1,3-benzothiazol-2-yl)cyclopropane-1-carboxamide
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C22H17N3OS
 1
1 Ki = 3500 nM
Clinical Information about the Protein
Target 1 ( T-cell-specific kinase (ITK) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Inflammation [ICD-11: 1A00-CA43.1]
Investigative Drug(s) 2 Investigative Drugs  2
1 BMS-488516 Investigative
Inflammation
2 BMS-509744 Investigative
Inflammation
Target 2 ( Tyrosine-protein kinase ITK (ITK) )
Target Type Literature-reported Target