The Ligandable Human Proteome

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Serine/threonine-protein kinase pim-1

Protein kinase domain

IndexLigand NameStructurePDB codeCompound Potency nM
12hxPim1 Complexed with a pyridylcarboxamide4n700.001
21ocStructure of PIM-1 kinase bound to N-(5-(2-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-((((3R,4R)-3-fluoropiperidin-4-yl)methyl)amino)pyrazolo[1,5-a]pyrimidine-3-carboxamide4k1b0.003
35h7Identification of N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1,2 and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies5dwr0.006
45e6PIM1 in complex with Cpd36 ((1S,3S)-N1-(6-(5-(pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridin-3-yl)pyridin-2-yl)cyclohexane-1,3-diamine)5dia0.035
56ynCrystal structure of human Pim-1 kinase in complex with an imidazopyridazine inhibitor.5kzi0.1
63u1Crystal structure of human Pim-1 kinase in complex with an azaspiro pyrazinyl-indazole inhibitor.4wrs0.4
70f5Exploitation of hydrogen bonding constraints and flat hydrophobic energy landscapes in Pim-1 kinase needle screening and inhibitor design3vbq0.47
8lxgDiscovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as Potent, Highly Selective and Orally Bioavailable Pim Kinases Inhibitors3jxw1
9unmThe discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors3r021
106cbDesign, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl-amide scaffold5iis1
111obStructure of PIM-1 kinase bound to 5-(4-cyanobenzyl)-N-(4-fluorophenyl)-7-hydroxypyrazolo[1,5-a]pyrimidine-3-carboxamide4k181.1
1226lDiscovery of Pyrazolo[1,5a]pyrimidine-based Pim1 Inhibitors4mbl2.9
1355eCrystal structure of human Pim1 kinase complexed with 4-(4-hydroxy-3-methyl-phenyl)-6-phenylpyrimidin-2(1H)-one3dcv3
14596Crystal structure of Pim1 kinase in complex with inhibitor (Z)-2-[(1H-indazol-3-yl)methylene]-6-methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one3umw3
157liNovel and selective pan-PIM kinase inhibitor4dtk3
16lygDiscovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as Potent, Highly Selective and Orally Bioavailable Pim Kinases Inhibitors3jy05
173yrPIM1 kinase in complex with Compound 1s4xhk5
18r9pBenzofuropyrimidinone Inhibitors of Pim-14alv7
1926kDiscovery of Pyrazolo[1,5a]pyrimidine-based Pim1 Inhibitors4mbi7
20vx2Human Pim-1 kinase in complex with an triazolo pyridazine inhibitor VX23bgq11
213u6Crystal structure of human Pim-1 kinase in complex with a thiadiazolamine-indole inhibitor.4wt612
22676Crystal structure of PIM1 in complex with a Pyrrolo-Pyrazinone inhibitor4bzo13
23l20Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors5dgz14
241oaStructure of PIM-1 kinase bound to N-(4-fluorophenyl)-7-hydroxy-5-(piperidin-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide4k0y15
252hwPim1 Complexed with a pyridylcarboxamide4n6z16
2679oBenzofuropyrimidinone Inhibitors of Pim-14alu17
27hy7Benzofuropyrimidinone Inhibitors of Pim-14alw27
28xj1Protein kinase Pim-1 in complex with small molecule inibitor2xj128
29queCrystal structure of Pim1 in complex with the inhibitor Quercetin (resulting from displacement of SKF86002)4lmu55
30985Crystal structure of human Pim-1 in complex with DAPPA3f2a57
31985Protein kinase Pim-1 in complex with small molecule inhibitor2xj266
322hvPim1 Complexed with a phenylcarboxamide4n6y92
33unqThe discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors3r04120
341n6Crystal structure of Pim1 kinase in complex with inhibitor 2-[(trans-4-aminocyclohexyl)amino]-4-{[3-(trifluoromethyl)phenyl]amino}pyrido[4,3-d]pyrimidin-5(6H)-one4jx7123
35q17Crystal structure of Pim1 in complex with 2-{4-[(3-aminopropyl)amino]quinazolin-2-yl}phenol (resulting from displacement of SKF86002)4lm5150
36q17Crystal structure of Pim1 kinase in complex with small molecule inhibitor3uix151
376s3Pim-1 kinase in Complex with a Selective N-substituted 7-azaindole Inhibitor5kcx200
383ngCrystal structure of PIM1 kinase in complex with small-molecule inhibitor5o11216
39myuCrystal structure of Pim1 with Quercetagetin2o64340
407auPim-1 kinase in complex with a 7-azaindole5tex400
41c2jPim1 complexed with N-(6-(4-hydroxyphenyl)-1H-indazol-3-yl)cyclopropanecarboxamide6ayd500
42queCrystal structure of Pim1 with Quercetin2o3p1100
43ugxCrystal structure of PIM1 in complex with a Pyrrolo(1,2-a)Pyrazinone inhibitor4bzn1441
44hulCrystal structure of proto-oncogene kinase Pim1 bound to hispidulin4xh62710