General Information of the Protein
Protein ID
PT01017
Protein Name
Serine/threonine-protein kinase pim-1
Gene Name
PIM1
Sequence
MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSDNLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLILERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDIPFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETAEIHLHSLSPGPSK
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CAMK protein kinase group
>
CAMK protein kinase PIM family
Function
Proto-oncogene with serine/threonine kinase activity involved in cell survival and cell proliferation and thus providing a selective advantage in tumorigenesis (PubMed:15528381, PubMed:1825810, PubMed:31548394). Exerts its oncogenic activity through: the regulation of MYC transcriptional activity, the regulation of cell cycle progression and by phosphorylation and inhibition of proapoptotic proteins (BAD, MAP3K5, FOXO3) (PubMed:18593906). Phosphorylation of MYC leads to an increase of MYC protein stability and thereby an increase of transcriptional activity (By similarity). The stabilization of MYC exerted by PIM1 might explain partly the strong synergism between these two oncogenes in tumorigenesis (By similarity). Mediates survival signaling through phosphorylation of BAD, which induces release of the anti-apoptotic protein Bcl-X(L)/BCL2L1 (By similarity). Phosphorylation of MAP3K5, another proapoptotic protein, by PIM1, significantly decreases MAP3K5 kinase activity and inhibits MAP3K5-mediated phosphorylation of JNK and JNK/p38MAPK subsequently reducing caspase-3 activation and cell apoptosis (PubMed:19749799). Stimulates cell cycle progression at the G1-S and G2-M transitions by phosphorylation of CDC25A and CDC25C (PubMed:16356754). Phosphorylation of CDKN1A, a regulator of cell cycle progression at G1, results in the relocation of CDKN1A to the cytoplasm and enhanced CDKN1A protein stability (PubMed:12431783). Promotes cell cycle progression and tumorigenesis by down-regulating expression of a regulator of cell cycle progression, CDKN1B, at both transcriptional and post-translational levels (PubMed:18593906). Phosphorylation of CDKN1B, induces 14-3-3 proteins binding, nuclear export and proteasome-dependent degradation (PubMed:18593906). May affect the structure or silencing of chromatin by phosphorylating HP1 gamma/CBX3 (PubMed:10664448). Acts also as a regulator of homing and migration of bone marrow cells involving functional interaction with the CXCL12-CXCR4 signaling axis (By similarity). Acts as a positive regulator of mTORC1 signaling by mediating phosphorylation and inhibition of DEPDC5 component of the GATOR1 complex (PubMed:31548394). Also phosphorylates and activates the ATP-binding cassette transporter ABCG2, allowing resistance to drugs through their excretion from cells (PubMed:18056989). Promotes brown adipocyte differentiation (By similarity).
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Uniprot ID
Primary ID:
P11309

Secondarily ID:
Q38RT9
Q5T7H7
Q96RG3
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Ensembl ID
ENSG00000137193
HGNC ID
HGNC:8986
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: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0561634
US9434725, 122
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C23H25N7O
 1
1
IC50 = 71.5 nM
   TI
   LI
   LO
   TS
CP0393246
US9434725, 168
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C20H20N8
 1
1
IC50 = 75.5 nM
   TI
   LI
   LO
   TS
CP0564892
US9434725, 172
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C22H24N8O
 1
1
IC50 = 111 nM
   TI
   LI
   LO
   TS
CP0567653
US9434725, 285
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C21H23N9
 1
1
IC50 = 112 nM
   TI
   LI
   LO
   TS
CP0478323
US9434725, 306
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C21H19F4N7
 1
1
IC50 = 129 nM
   TI
   LI
   LO
   TS
CP0479633
US9434725, 165
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C22H22N8
 1
1
IC50 = 139 nM
   TI
   LI
   LO
   TS
CP0513361
US9434725, 282
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C21H23N9O
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0578206
US9434725, 208
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C21H23N9
 1
1
IC50 = 173 nM
   TI
   LI
   LO
   TS
CP0419275
US9434725, 162
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C21H22F2N8
 1
1
IC50 = 175 nM
   TI
   LI
   LO
   TS
CP0516120
US9434725, 189
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C21H21F3N8O
 1
1
IC50 = 181 nM
   TI
   LI
   LO
   TS
CP0532564
US9434725, 150
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C22H24N8
 1
1
IC50 = 196 nM
   TI
   LI
   LO
   TS
CP0516406
US9434725, 218
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C22H24N8O
 1
1
IC50 = 212 nM
   TI
   LI
   LO
   TS
CP0578203
US9434725, 181
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C24H26N8
 1
1
IC50 = 214 nM
   TI
   LI
   LO
   TS
CP0085927
US9434725, 186
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C22H24N8O
 1
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0483229
US9434725, 190
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C21H22N8
 1
1
IC50 = 235 nM
   TI
   LI
   LO
   TS
CP0512362
US9434725, 313
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C19H19N9
 1
1
IC50 = 236 nM
   TI
   LI
   LO
   TS
CP0518526
US9434725, 149
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C21H22N8
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0478322
US9434725, 304
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C20H19N7O
 1
1
IC50 = 255 nM
   TI
   LI
   LO
   TS
CP0471270
US9434725, 278
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C21H22N8O2
 1
1
IC50 = 261 nM
   TI
   LI
   LO
   TS
CP0479634
US9434725, 166
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C21H21N7
 1
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0451558
US9434725, 174
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C22H24N8
 1
1
IC50 = 271 nM
   TI
   LI
   LO
   TS
CP0567651
US9434725, 205
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C22H24N8
 1
1
IC50 = 278 nM
   TI
   LI
   LO
   TS
CP0406605
US9434725, 123
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C20H20N8
 1
1
IC50 = 284 nM
   TI
   LI
   LO
   TS
CP0465859
US9434725, 153
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C21H23FN8
 1
1
IC50 = 291 nM
   TI
   LI
   LO
   TS
CP0539934
US9434725, 154
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C21H21F3N8
 1
1
IC50 = 344 nM
   TI
   LI
   LO
   TS
CP0479635
US9434725, 179
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C20H20F3N9
 1
1
IC50 = 376 nM
   TI
   LI
   LO
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CP0488613
US9434725, 260
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C22H23F3N8O
 1
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0515240
US9434725, 284
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C22H23N9
 1
1
IC50 = 385 nM
   TI
   LI
   LO
   TS
CP0529004
US9434725, 144
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C19H18N8
 1
1
IC50 = 385 nM
   TI
   LI
   LO
   TS
CP0578204
US9434725, 188
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C21H21F3N8O
 1
1
IC50 = 418 nM
   TI
   LI
   LO
   TS
CP0565323
US9434725, 295
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C22H23N7O
 1
1
IC50 = 425 nM
   TI
   LI
   LO
   TS
CP0445039
US9434725, 112
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C24H25N7
 1
1
IC50 = 490 nM
   TI
   LI
   LO
   TS
CP0575914
US9434725, 201
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C22H21N9
 1
1
IC50 = 490 nM
   TI
   LI
   LO
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CP0497624
US9434725, 155
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C21H21N9
 1
1
IC50 = 518 nM
   TI
   LI
   LO
   TS
CP0393247
US9434725, 176
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C21H21ClN8
 1
1
IC50 = 533 nM
   TI
   LI
   LO
   TS
CP0419273
US9434725, 151
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C21H22N8O
 1
1
IC50 = 544 nM
   TI
   LI
   LO
   TS
CP0549620
US9434725, 167
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C20H20N8
 1
1
IC50 = 546 nM
   TI
   LI
   LO
   TS
CP0515238
US9434725, 178
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C20H20F3N9
 1
1
IC50 = 549 nM
   TI
   LI
   LO
   TS
CP0483230
US9434725, 196
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C21H22N8
 1
1
IC50 = 572 nM
   TI
   LI
   LO
   TS
CP0110430
US9434725, 138
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C21H22N8
 1
1
IC50 = 574 nM
   TI
   LI
   LO
   TS
CP0563781
US9434725, 279
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C20H18F2N8
 1
1
IC50 = 622 nM
   TI
   LI
   LO
   TS
CP0483233
US9434725, 273
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C20H20N8O
 1
1
IC50 = 629 nM
   TI
   LI
   LO
   TS
CP0564894
US9434725, 307
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C20H20N8
 1
1
IC50 = 640 nM
   TI
   LI
   LO
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CP0483232
US9434725, 209
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C21H23N9
 1
1
IC50 = 682 nM
   TI
   LI
   LO
   TS
CP0483234
US9434725, 281
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C22H23N9O
 1
1
IC50 = 695 nM
   TI
   LI
   LO
   TS
CP0554650
US9434725, 216
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C24H26N8
 1
1
IC50 = 715 nM
   TI
   LI
   LO
   TS
CP0393248
US9434725, 180
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C19H20N8
 1
1
IC50 = 745 nM
   TI
   LI
   LO
   TS
CP0566379
US9434725, 274
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C21H20N8
 1
1
IC50 = 749 nM
   TI
   LI
   LO
   TS
CP0564882
US9434725, 294
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C21H20FN7
 1
1
IC50 = 772 nM
   TI
   LI
   LO
   TS
CP0567652
US9434725, 228
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C21H23N9
 1
1
IC50 = 778 nM
   TI
   LI
   LO
   TS
CP0563393
US9434725, 301
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C22H24N8O
 1
1
IC50 = 781 nM
   TI
   LI
   LO
   TS
CP0495376
US9434725, 146
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C22H26N8
 1
1
IC50 = 797 nM
   TI
   LI
   LO
   TS
CP0564470
US9434725, 124
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C20H21N7S
 1
1
IC50 = 804 nM
   TI
   LI
   LO
   TS
CP0514648
US9434725, 225
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C21H20N8O
 1
1
IC50 = 840 nM
   TI
   LI
   LO
   TS
CP0515239
US9434725, 227
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C22H22F2N8
 1
1
IC50 = 869 nM
   TI
   LI
   LO
   TS
CP0530438
US9434725, 147
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C23H26N8
 1
1
IC50 = 869 nM
   TI
   LI
   LO
   TS
CP0393254
US9434725, 277
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C21H22N8O2
 1
1
IC50 = 912 nM
   TI
   LI
   LO
   TS
CP0469600
US9434725, 191
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C21H22N8
 1
1
IC50 = 919 nM
   TI
   LI
   LO
   TS
CP0564064
US9434725, 187
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C22H24N8
 1
1
IC50 = 963 nM
   TI
   LI
   LO
   TS
CP0512361
US9434725, 293
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C23H24N8
 1
1
IC50 = 976 nM
   TI
   LI
   LO
   TS
CP0393253
US9434725, 214
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C22H22N8
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0445042
US9434725, 141
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C22H23N7
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0513362
US9434725, 283
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C24H27N9O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0563782
US9434725, 317
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C22H20N8
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0393250
US9434725, 198
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C21H21FN8
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0565321
US9434725, 184
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C22H24N8
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0471272
US9434725, 297
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C17H15N7
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0497619
US9434725, 106
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C23H25N7O
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0530436
US9434725, 103
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C24H27N7
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0564878
US9434725, 215
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C21H21FN8
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0564880
US9434725, 220
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C22H21F3N8
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0515254
US9434725, 308
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C18H16N8
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0576939
US9434725, 300
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C22H20N8O
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0497625
US9434725, 156
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C22H24N8
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0561635
US9434725, 125
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C21H24N8
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0564469
US9434725, 120
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C20H21N7S
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0393251
US9434725, 207
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C22H24N8O2
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0481144
US9434725, 194
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C21H22N8
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0481145
US9434725, 224
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C20H22N8
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0497620
US9434725, 130
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C20H20N8O
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0559292
US9434725, 152
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C21H24N8O
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0563439
US9434725, 109
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C18H17N7S
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0564468
US9434725, 104
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C22H23N7
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0499635
US9434725, 105
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C23H25N7
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0513363
US9434725, 299
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C21H21N7O
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0536004
US9434725, 298
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C21H21N7O
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0532642
US9434725, 101
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C20H22N8
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0565735
US9434725, 110
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C19H19N7S
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0575913
US9434725, 192
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C21H21FN8
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0576940
US9434725, 315
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C21H18N8
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0497621
US9434725, 137
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C21H22N8
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0578205
US9434725, 197
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C24H26N8
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0500959
US9434725, 139
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C26H29N7
 1
1
IC50 = 2300 nM
   TI
   LI
   LO
   TS
CP0529051
US9434725, 107
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C24H27N7
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0497623
US9434725, 145
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C23H28N8
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0563458
US9434725, 157
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C22H26N8O2S
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0530437
US9434725, 117
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C23H24ClN7
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0445040
US9434725, 133
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C21H24N8
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0488614
US9434725, 296
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C18H17N7
 1
1
IC50 = 3800 nM
   TI
   LI
   LO
   TS
CP0563392
US9434725, 286
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C21H23N9O
 1
1
IC50 = 4200 nM
   TI
   LI
   LO
   TS
CP0495375
US9434725, 108
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C24H27N7
 1
1
IC50 = 4500 nM
   TI
   LI
   LO
   TS
CP0564893
US9434725, 302
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C22H22N8O
 1
1
IC50 = 6100 nM
   TI
   LI
   LO
   TS
CP0483235
US9434725, 303
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C22H22N8O
 1
1
IC50 = 6600 nM
   TI
   LI
   LO
   TS
CP0483236
US9434725, 316
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C21H22FN7
 1
1
IC50 > 25000 nM
   TI
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   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0391702
(2Z)-2-[(6-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methylidene]-6-methoxy-7-(piperazin-1-ylmethyl)-1-benzofuran-3-one
   Show/Hide
C22H21ClN4O3
 1
1 IC50 = 0.41 nM
CP0315758
3,4-dichloro-2-(2-cyclopropylethynyl)-1-piperidin-3-ylpyrrolo[2,3-b]pyridine-6-carboxamide
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C18H18Cl2N4O
 1
1 IC50 = 0.7 nM
CP0069651
7-methoxy-N-(piperidin-4-ylmethyl)-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C19H21F3N6O2
 1
1 IC50 = 1 nM
CP0237490
5-[3-[6-(cyclopentylamino)pyrazin-2-yl]-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C19H19N7S
 1
1 IC50 = 1 nM
CP0110066
3,4-dichloro-2-cyclopropyl-1-[(3S)-piperidin-3-yl]pyrrolo[2,3-b]pyridine-6-carboxamide
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C16H18Cl2N4O
 1
1 IC50 = 1 nM
CP0315757
3,4-dichloro-2-iodo-1-piperidin-3-ylpyrrolo[2,3-b]pyridine-6-carboxamide
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C13H13Cl2IN4O
 1
1 IC50 = 1 nM
CP0540245
3,4-dichloro-2-cyclopropyl-1-piperidin-3-ylpyrrolo[2,3-b]pyridine-6-carboxamide
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C16H18Cl2N4O
 1
1 IC50 = 1 nM
CP0391701
(2Z)-2-[(6-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methylidene]-6-hydroxy-7-(piperazin-1-ylmethyl)-1-benzofuran-3-one
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C21H19ClN4O3
 1
1 IC50 = 1.4 nM
CP0128906
3-[3-(dimethylamino)phenyl]-7-methoxy-N-(piperidin-4-ylmethyl)triazolo[4,5-b]pyridin-5-amine
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C20H27N7O
 1
1 IC50 = 1.5 nM
CP0263622
5-[3-[6-(propan-2-ylamino)pyrazin-2-yl]-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C17H17N7S
 1
1 IC50 = 2 nM
CP0126602
N-(7-azaspiro[3.5]nonan-2-ylmethyl)-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C21H23F3N6O
 1
1 IC50 = 4 nM
CP0089230
5-[3-[6-(cyclohexylamino)pyrazin-2-yl]-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C20H21N7S
 1
1 IC50 = 4 nM
CP0306649
7-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(piperidin-4-ylmethyl)isoquinolin-1-amine
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C23H26N8O
 1
1 IC50 = 4 nM
CP0126600
3-[3-(dimethylamino)phenyl]-N-(piperidin-4-ylmethyl)triazolo[4,5-b]pyridin-5-amine
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C19H25N7
 1
1 IC50 = 5 nM
CP0088414
5-[3-(6-morpholin-4-ylpyrazin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C18H17N7OS
 1
1 IC50 = 5 nM
CP0110465
6-chloro-N-(piperidin-4-ylmethyl)-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C18H18ClF3N6O
 1
1 IC50 = 6 nM
CP0200067
N-(piperidin-4-ylmethyl)-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C18H19F3N6O
 1
1 IC50 = 6 nM
CP0165556
7-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(piperidin-4-ylmethyl)naphthalen-1-amine
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C24H27N7O
 1
1 IC50 = 6 nM
CP0070817
N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
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C20H22F3N5O
 8
1 IC50 = 7 nM
2 IC50 = 7.6 nM
3 IC50 = 13 nM
4 IC50 = 20 nM
5 IC50 = 46 nM
6 IC50 = 48 nM
7 Ki = 12 nM
8 Ki = 16 nM
CP0713718
N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine disulfate
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C20H24F3N5O5S
 1
1 IC50 = 7 nM
CP0116608
5-[3-(6-propan-2-yloxypyridin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C18H17N5OS
 1
1 IC50 = 7 nM
CP0139015
N-[(4-fluoropiperidin-4-yl)methyl]-7-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)isoquinolin-1-amine
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C23H25FN8O
 1
1 IC50 = 7 nM
CP0139017
2-[10-(2-methoxyethyl)-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl]-N-(piperidin-4-ylmethyl)quinolin-8-amine
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C25H30N8O2
 1
1 IC50 = 7 nM
CP0165554
2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(1-methylpiperidin-4-yl)quinolin-8-amine
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C23H26N8O
 1
1 IC50 = 7 nM
CP0116609
5-[3-(6-propan-2-yloxypyrazin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C17H16N6OS
 1
1 IC50 = 8 nM
CP0126603
N-(7-azaspiro[3.5]nonan-2-ylmethyl)-3-[3-(trifluoromethyl)phenyl]triazolo[4,5-b]pyridin-5-amine
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C21H23F3N6
 1
1 IC50 = 9 nM
CP0551450
6-fluoro-N-[(4-fluoropiperidin-4-yl)methyl]-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C23H24F2N8O
 1
1 IC50 = 10 nM
CP0090814
N-(7-azaspiro[3.5]nonan-2-yl)-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C20H21F3N6O
 1
1 IC50 = 11 nM
CP0073954
5-[3-(6-pyrrolidin-1-ylpyrazin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C18H17N7S
 1
1 IC50 = 11 nM
CP0111732
5-[3-(6-cyclopentyloxypyrazin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C19H18N6OS
 1
1 IC50 = 11 nM
CP0089234
5-[3-[6-(cyclopentylamino)pyridin-2-yl]-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C20H20N6S
 1
1 IC50 = 12 nM
CP0139020
2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-piperidin-4-ylquinolin-8-amine
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C22H24N8O
 1
1 IC50 = 12 nM
CP0139024
7-chloro-N-[(4-fluoropiperidin-4-yl)methyl]-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C23H24ClFN8O
 1
1 IC50 = 12 nM
CP0365953
N-(piperidin-4-ylmethyl)-2-(10-propyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C25H30N8O
 1
1 IC50 = 12 nM
CP0134290
2-(10-ethyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(piperidin-4-ylmethyl)quinolin-8-amine
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C24H28N8O
 1
1 IC50 = 13 nM
CP0323040
N-(7-azaspiro[3.5]nonan-2-yl)-3-[3-(trifluoromethyl)phenyl]triazolo[4,5-b]pyridin-5-amine
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C20H21F3N6
 1
1 IC50 = 14 nM
CP0134292
2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-[(1-methylpiperidin-4-yl)methyl]quinolin-8-amine
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C24H28N8O
 1
1 IC50 = 14 nM
CP0177610
2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(piperidin-4-ylmethyl)quinolin-8-amine
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C23H26N8O
 1
1 IC50 = 14 nM
CP0114265
5-[3-(6-cyclopentyloxypyridin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C20H19N5OS
 1
1 IC50 = 15 nM
CP0089229
5-[3-(6-morpholin-4-ylpyridin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C19H18N6OS
 1
1 IC50 = 16 nM
CP0139018
N-(piperidin-4-ylmethyl)-2-(10-propan-2-yl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C25H30N8O
 1
1 IC50 = 16 nM
CP0126713
CHEMBL1952132
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C18H18F3N5O2
 1
1 IC50 = 17 nM
CP0116606
5-[3-(6-ethoxypyridin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C17H15N5OS
 1
1 IC50 = 17 nM
CP0365952
2-[10-(2-phenoxyethyl)-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl]-N-(piperidin-4-ylmethyl)quinolin-8-amine
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C30H32N8O2
 1
1 IC50 = 17 nM
CP0140103
5,6-difluoro-N-[(4-fluoropiperidin-4-yl)methyl]-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C23H23F3N8O
 1
1 IC50 = 18 nM
CP0126118
N'-[6-[6-(propan-2-ylamino)indazol-1-yl]pyrazin-2-yl]propane-1,3-diamine
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C17H23N7
 1
1 IC50 = 20 nM
CP0089231
5-[3-(6-ethoxypyrazin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C16H14N6OS
 1
1 IC50 = 21 nM
CP0134289
N-[(4-fluoropiperidin-4-yl)methyl]-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C23H25FN8O
 1
1 IC50 = 21 nM
CP0177178
5-[3-[6-(propan-2-ylamino)pyridin-2-yl]-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C18H18N6S
 1
1 IC50 = 24 nM
CP0140122
2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(oxan-4-yl)quinolin-8-amine
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C22H23N7O2
 1
1 IC50 = 25 nM
CP0165564
N-cyclohexyl-7-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)isoquinolin-1-amine
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C23H25N7O
 1
1 IC50 = 26 nM
CP0164528
CHEMBL1952133
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C18H18F3N5O2
 1
1 IC50 = 27 nM
CP0139025
5-fluoro-N-[(4-fluoropiperidin-4-yl)methyl]-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C23H24F2N8O
 1
1 IC50 = 30 nM
CP0160159
2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)-N-(oxan-4-ylmethyl)quinolin-8-amine
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C23H25N7O2
 1
1 IC50 = 30 nM
CP0306648
N-cyclohexyl-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C23H25N7O
 1
1 IC50 = 32 nM
CP0352349
N-[2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-yl]piperidine-4-carboxamide
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C23H24N8O2
 1
1 IC50 = 36 nM
CP0282932
N-piperidin-4-yl-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C17H17F3N6O
 1
1 IC50 = 38 nM
CP0139013
1-[2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-yl]piperidin-4-amine
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C22H24N8O
 1
1 IC50 = 38 nM
CP0073948
5-[3-(6-cyclohexyloxypyridin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C21H21N5OS
 1
1 IC50 = 41 nM
CP0140104
N-cyclohexyl-7-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)naphthalen-1-amine
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C24H26N6O
 1
1 IC50 = 46 nM
CP0089233
5-[3-(6-pyrrolidin-1-ylpyridin-2-yl)-1H-indol-5-yl]-1,3,4-thiadiazol-2-amine
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C19H18N6S
 1
1 IC50 = 48 nM
CP0089232
5-(3-quinolin-3-yl-1H-indol-5-yl)-1,3,4-thiadiazol-2-amine
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C19H13N5S
 1
1 IC50 = 163 nM
CP0240841
3-fluoro-4-[6-[6-(propan-2-ylamino)indazol-1-yl]pyrazin-2-yl]benzoic acid
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C21H18FN5O2
 1
1 IC50 = 200 nM
CP0177609
10-methyl-5-(8-piperazin-1-ylquinolin-2-yl)-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraene
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C21H22N8O
 1
1 IC50 = 200 nM
CP0365954
N-[(4-fluoropiperidin-4-yl)methyl]-6-methyl-2-(10-methyl-13-oxa-3,4,6,7,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7-tetraen-5-yl)quinolin-8-amine
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C24H27FN8O
 1
1 IC50 = 236 nM
CP0085927
US9434725, 186
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C22H24N8O
 1
1 Ki = 0.018 nM
CP0110430
US9434725, 138
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C21H22N8
 1
1 Ki = 0.02 nM
Clinical Information about the Protein
Target 1 ( Serine/threonine-protein kinase pim-1 (PIM1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Non-small-cell lung cancer [ICD-11: 2C25]
Investigative Drug(s) 1 Investigative Drug  1
1 SMI-4a Investigative
Non-small-cell lung cancer