The Ligandable Human Proteome

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Tyrosine-protein kinase ITK/TSK

Protein kinase domain

IndexLigand NameStructurePDB codeCompound Potency nM
13p6ITK kinase domain in complex with compound 1 N-{1-[(1,1-dioxo-1-thian-2-yl)(phenyl)methyl]-1H- pyrazol-4-yl}-5,5-difluoro-5a-methyl-1H,4H,4aH,5H,5aH,6H-cyclopropa[f]indazole-3-carboxamide4rfm0.09
22vvITK kinase domain with compound 28 (N-{1-[(1S)-3-(DIMETHYLAMINO)-1-PHENYLPROPYL]-1H-PYRAZOL-4-YL}-6-(1H-PYRAZOL-4-YL)-1H-INDAZOLE-3-CARBOXAMIDE)4ppb0.1
329yITK kinase domain in complex with benzothiazole inhibitor 12b (1S,2S)-2-{4-[(DIMETHYLAMINO)METHYL]PHENYL}-N-[6-(1H-PYRAZOL-4-YL)-1,3-BENZOTHIAZOL-2-YL]CYCLOPROPANECARBOXAMIDE4mf10.7
42w6ITK kinase domain with compound GNE-98224pqn0.7
52vuITK kinase domain with compound 11 (N-[1-(3-CYANOBENZYL)-1H-PYRAZOL-4-YL]-6-(1H-PYRAZOL-4-YL)-1H-INDAZOLE-3-CARBOXAMIDE)4ppa0.8
62vwITK kinase domain with compound 27 (N-{1-[(1R)-3-(DIMETHYLAMINO)-1-PHENYLPROPYL]-1H-PYRAZOL-4-YL}-6-(1H-PYRAZOL-4-YL)-1H-INDAZOLE-3-CARBOXAMIDE)4ppc0.93
7iaqCrystal structure of BTK mutant (F435T,K596R) complexed with Imidazo[1,5-a]quinoxaline3t9t1.93
813lCrystal structure of ITK in complext with compound 404hcu10
90f2Crystal Structure of Interleukin-2 Inducible T-cell Kinase Itk Catalytic Domain with Thienopyrazolylindole Inhibitor 0903v5j10.9
10mjgX-ray crystal structure of ITK complexed with inhibitor BMS-5097443mj215
11614X-ray crystal structure of ITK complexed with inhibitor RO51916143mj115
12b49X-ray crystal structure of ITK complexed with sunitinib3miy21
132vtITK kinase domain with compound 1 (N-[1-(3-CYANOBENZYL)-1H-PYRAZOL-4-YL]-2H-INDAZOLE-3-CARBOXAMIDE)4pp943
1418rCrystal structure of ITK in complex with compound 524hct73
151e0Crystal structure of ITK in complex with compound 8 [4-(carbamoylamino)-1-(7-propoxynaphthalen-1-yl)-1H-pyrazole-3-carboxamide]4m13200
1613jCrystal structure of ITK in complex with compound 534hcv400
17g5kKinase domain mutant of human Itk in complex with a covalently-binding inhibitor4kio501
181yzCrystal structure of ITK in complex with compound 7 [4-(carbamoylamino)-1-(7-ethoxynaphthalen-1-yl)-1H-pyrazole-3-carboxamide]4m12900
19m0zCrystal structure of ITK in complex with compound 5 {4-(carbamoylamino)-1-(7-methoxynaphthalen-1-yl)-1H-pyrazole-3-carboxamide}4m0z6400