General Information of the Protein
Protein ID
PT01235
Protein Name
Cyclin-dependent kinase 9
Secondarily
Protein Name
C-2K
Cell division cycle 2-like protein kinase 4
Cell division protein kinase 9
Serine/threonine-protein kinase PITALRE
Tat-associated kinase complex catalytic subunit
Gene Name
CDK9
Secondarily
Gene Name
CDC2L4
TAK
Sequence
MAKQYDSVECPFCDEVSKYEKLAKIGQGTFGEVFKARHRKTGQKVALKKVLMENEKEGFPITALREIKILQLLKHENVVNLIEICRTKASPYNRCKGSIYLVFDFCEHDLAGLLSNVLVKFTLSEIKRVMQMLLNGLYYIHRNKILHRDMKAANVLITRDGVLKLADFGLARAFSLAKNSQPNRYTNRVVTLWYRPPELLLGERDYGPPIDLWGAGCIMAEMWTRSPIMQGNTEQHQLALISQLCGSITPEVWPNVDNYELYEKLELVKGQKRKVKDRLKAYVRDPYALDLIDKLLVLDPAQRIDSDDALNHDFFWSDPMPSDLKGMLSTHLTSMFEYLAPPRRKGSQITQQSTNQSRNPATTNQTEFERVF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase CDK family
>
CMGC protein kinase CDK9 subfamily
Function
Protein kinase involved in the regulation of transcription (PubMed:10574912, PubMed:10757782, PubMed:11145967, PubMed:11575923, PubMed:11809800, PubMed:11884399, PubMed:14701750, PubMed:16109376, PubMed:16109377, PubMed:20930849, PubMed:28426094, PubMed:29335245). Member of the cyclin-dependent kinase pair (CDK9/cyclin-T) complex, also called positive transcription elongation factor b (P-TEFb), which facilitates the transition from abortive to productive elongation by phosphorylating the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAP II) POLR2A, SUPT5H and RDBP (PubMed:10574912, PubMed:10757782, PubMed:11145967, PubMed:11575923, PubMed:11809800, PubMed:11884399, PubMed:14701750, PubMed:16109376, PubMed:16109377, PubMed:20930849, PubMed:28426094, PubMed:30134174). This complex is inactive when in the 7SK snRNP complex form (PubMed:10574912, PubMed:10757782, PubMed:11145967, PubMed:11575923, PubMed:11809800, PubMed:11884399, PubMed:14701750, PubMed:16109376, PubMed:16109377, PubMed:20930849, PubMed:28426094). Phosphorylates EP300, MYOD1, RPB1/POLR2A and AR and the negative elongation factors DSIF and NELFE (PubMed:9857195, PubMed:10912001, PubMed:11112772, PubMed:12037670, PubMed:20081228, PubMed:20980437, PubMed:21127351). Regulates cytokine inducible transcription networks by facilitating promoter recognition of target transcription factors (e.g. TNF-inducible RELA/p65 activation and IL-6-inducible STAT3 signaling) (PubMed:17956865, PubMed:18362169). Promotes RNA synthesis in genetic programs for cell growth, differentiation and viral pathogenesis (PubMed:10393184, PubMed:11112772). P-TEFb is also involved in cotranscriptional histone modification, mRNA processing and mRNA export (PubMed:15564463, PubMed:19575011, PubMed:19844166). Modulates a complex network of chromatin modifications including histone H2B monoubiquitination (H2Bub1), H3 lysine 4 trimethylation (H3K4me3) and H3K36me3; integrates phosphorylation during transcription with chromatin modifications to control co-transcriptional histone mRNA processing (PubMed:15564463, PubMed:19575011, PubMed:19844166). The CDK9/cyclin-K complex has also a kinase activity towards CTD of RNAP II and can substitute for CDK9/cyclin-T P-TEFb in vitro (PubMed:21127351). Replication stress response protein; the CDK9/cyclin-K complex is required for genome integrity maintenance, by promoting cell cycle recovery from replication arrest and limiting single-stranded DNA amount in response to replication stress, thus reducing the breakdown of stalled replication forks and avoiding DNA damage (PubMed:20493174). In addition, probable function in DNA repair of isoform 2 via interaction with KU70/XRCC6 (PubMed:20493174). Promotes cardiac myocyte enlargement (PubMed:20081228). RPB1/POLR2A phosphorylation on 'Ser-2' in CTD activates transcription (PubMed:21127351). AR phosphorylation modulates AR transcription factor promoter selectivity and cell growth. DSIF and NELF phosphorylation promotes transcription by inhibiting their negative effect (PubMed:9857195, PubMed:10912001, PubMed:11112772). The phosphorylation of MYOD1 enhances its transcriptional activity and thus promotes muscle differentiation (PubMed:12037670). Catalyzes phosphorylation of KAT5, promoting KAT5 recruitment to chromatin and histone acetyltransferase activity (PubMed:29335245).
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Uniprot ID
Primary ID:
P50750

Secondarily ID:
Q5JU24
Q5JU25
Q5U006
Q96TF1
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Ensembl ID
ENSG00000136807
HGNC ID
HGNC:1780
Subcellular Location
Nucleus
Cytoplasm
Nucleus
PML body
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: CL000052 , A-431
Compound ID Compound Name Compound Formula
CP0222241
US9073922, 87
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C19H18FN3O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0265963
US9073922, 101
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C21H20FN3O3
 1
1
IC50 = 72 nM
   TI
   LI
   LO
   TS
CP0143255
US9073922, 226
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C21H20FN3O3
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0341118
US9073922, 215
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C21H21FN4O2
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0726326
(1r,4r)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H27F2N3O3
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0965399
(1s,4s)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H27F2N3O3
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0962478
1-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperidine-4-carboxylic acid
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C27H29F2N3O3
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0968689
2-((1r,4r)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexyl)acetic acid
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C27H29F2N3O3
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0567168
US9796708, Example 228
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C22H23FN4O5S
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0773151
(1s,4s)-4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H28FN3O3
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0128822
US9073922, 288
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C27H30FN3O3
 1
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0265979
US9073922, 119
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C20H20FN3O3S
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0914334
(1r,4r)-4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H28FN3O3
 1
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0132970
US9073922, 289
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C27H30FN3O3
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0565903
US9073922, 241
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C25H28FN3O3
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0968691
2-(4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperazin-1-yl)acetic acid
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C26H29FN4O3
 1
1
IC50 = 640 nM
   TI
   LI
   LO
   TS
CP0961574
4-[4-(5-fluoro-2-methoxy-phenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-N-methylsulfonyl-cyclohex-3-ene-1-carboxamide
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C22H22FN3O4S
 1
1
IC50 = 660 nM
   TI
   LI
   LO
   TS
CP0962662
2-(1-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperidin-4-yl)acetic acid
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C26H28FN3O3
 1
1
IC50 = 680 nM
   TI
   LI
   LO
   TS
CP0965400
2-((1s,4s)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexyl)acetic acid
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C27H30FN3O3
 1
1
IC50 = 980 nM
   TI
   LI
   LO
   TS
CP0578436
(4-{4-[4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-3,6-dihydropyridin-1(2H)-yl}piperidin-1-yl)acetic acid
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C26H29FN4O3
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0963886
2-[[4-[4-(5-fluoro-2-methoxy-phenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]cyclohex-3-en-1-yl]amino]acetic acid
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C22H22FN3O3
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0697060
US9073922, 219
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C21H19FN2O3
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0968690
2-(4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperidin-1-yl)acetic acid
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C27H30FN3O3
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0699892
US9073922, 186
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C22H24FN3O3
 2
1 IC50 = 1.2 nM
2 IC50 = 4 nM
CP0726326
(1r,4r)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H27F2N3O3
 2
1 IC50 = 2.6 nM
2 IC50 = 78 nM
CP0002333
US9067888, 33
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C21H24FN3O3
 1
1 IC50 = 3 nM
CP0546232
5-(2-piperidin-4-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-propan-2-ylpyridin-2-one
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C20H24N4O
 1
1 IC50 < 3 nM
CP0551968
2-[4-[4-(4-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]ethanol
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C21H24FN3O2
 1
1 IC50 < 3 nM
CP0572890
N,N-dimethyl-2-[4-[4-(6-oxo-1-propan-2-ylpyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C24H31N5O2
 1
1 IC50 < 3 nM
CP0576423
N,N-dimethyl-2-[4-[4-(2-methyl-3-propan-2-ylbenzimidazol-5-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C27H34N6O
 1
1 IC50 < 3 nM
CP0119478
US9073922, 18
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C19H20FN3O
 3
1 IC50 < 3 nM
2 IC50 = 6 nM
3 IC50 = 19 nM
CP0545203
5-[2-[1-(2-oxo-2-piperidin-1-ylethyl)piperidin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-propan-2-ylpyridin-2-one
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C27H35N5O2
 3
1 IC50 < 3 nM
2 IC50 = 8 nM
3 Kd = 0.213 nM
CP0551967
[3-methoxy-4-(2-piperidin-4-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-pyrrolidin-1-ylmethanone
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C24H28N4O2
 2
1 IC50 < 3 nM
2 IC50 = 4 nM
CP0575262
5-[2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)piperidin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-propan-2-ylpyridin-2-one
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C26H33N5O2
 2
1 IC50 < 3 nM
2 IC50 = 6 nM
CP0579940
4-[[4-[4-(4-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]phenyl]methyl]morpholine
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C25H24FN3O2
 2
1 IC50 < 3 nM
2 IC50 = 16 nM
CP0006340
Dinaciclib
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C21H28N6O2
 3
1 IC50 < 3 nM
2 IC50 = 4 nM
3 IC50 = 178 nM
CP0003694
BMS-387072
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C17H24N4O2S2
 3
1 IC50 = 4 nM
2 Kd = 76 nM
3 Ki = 4 nM
CP0004075
(1S,3R)-3-acetamido-N-[5-chloro-4-(5,5-dimethyl-4,6-dihydropyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl]cyclohexane-1-carboxamide
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C22H28ClN5O2
 1
1 IC50 < 4 nM
CP0575344
N,N-dimethyl-2-[4-[4-(2-oxo-1-propan-2-ylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C23H30N6O2
 1
1 IC50 = 4 nM
CP0576422
[4-[2-[1-(2-hydroxyethyl)piperidin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-3-methoxyphenyl]-pyrrolidin-1-ylmethanone
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C26H32N4O3
 1
1 IC50 = 4 nM
CP0001372
(2R,3R)-3-[2-[4-(cyclopropylsulfonimidoyl)anilino]-5-(trifluoromethyl)pyrimidin-4-yl]oxybutan-2-ol
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C18H21F3N4O3S
 1
1 IC50 = 5 nM
CP0545348
2-[4-[4-(4-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]-N,N-dimethylacetamide
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C23H27FN4O2
 1
1 IC50 = 6 nM
CP0579964
N,N-dimethyl-2-[4-[4-(6-oxo-1-propan-2-ylpyridazin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C23H30N6O2
 1
1 IC50 = 8 nM
CP0575341
[3-methoxy-4-[2-[4-(morpholin-4-ylmethyl)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]phenyl]-pyrrolidin-1-ylmethanone
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C29H31N5O3
 2
1 IC50 = 9 nM
2 IC50 = 990 nM
CP0222241
US9073922, 87
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C19H18FN3O
 2
1 IC50 = 10 nM
2 IC50 = 14 nM
CP0351134
US9073922, 29
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C20H22FN3O
 2
1 IC50 = 10 nM
2 IC50 = 23 nM
CP0546231
N-methyl-2-[4-[4-(6-oxo-1-propan-2-ylpyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C23H29N5O2
 1
1 IC50 = 10 nM
CP0575342
N,N-dimethyl-2-[4-[4-(1-methyl-6-oxopyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C22H27N5O2
 2
1 IC50 = 10 nM
2 IC50 = 1000 nM
CP0575343
N,N-dimethyl-2-[4-[4-[1-(2-methylsulfanylethyl)-6-oxopyridin-3-yl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C24H31N5O2S
 1
1 IC50 = 11 nM
CP0579941
1-[4-[4-[2-methoxy-4-(pyrrolidine-1-carbonyl)phenyl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]ethanone
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C26H30N4O3
 1
1 IC50 = 11 nM
CP0572977
1-propan-2-yl-5-[2-[1-(thiophen-2-ylmethyl)piperidin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]pyridin-2-one
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C25H28N4OS
 1
1 IC50 = 14 nM
CP0341118
US9073922, 215
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C21H21FN4O2
 2
1 IC50 = 19 nM
2 IC50 = 21 nM
CP0567168
US9796708, Example 228
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C22H23FN4O5S
 1
1 IC50 = 25 nM
CP0143255
US9073922, 226
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C21H20FN3O3
 1
1 IC50 = 33 nM
CP0265963
US9073922, 101
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C21H20FN3O3
 1
1 IC50 = 36 nM
CP0265979
US9073922, 119
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C20H20FN3O3S
 2
1 IC50 = 37 nM
2 IC50 = 43 nM
CP0576424
5-[2-(1-acetylpiperidin-4-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-propan-2-ylpyridin-2-one
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C22H26N4O2
 1
1 IC50 = 39 nM
CP0132970
US9073922, 289
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C27H30FN3O3
 2
1 IC50 = 57 nM
2 IC50 = 200 nM
CP0577930
[3-methoxy-4-[2-(oxan-4-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-pyrrolidin-1-ylmethanone
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C24H27N3O3
 1
1 IC50 = 57 nM
CP0697060
US9073922, 219
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C21H19FN2O3
 2
1 IC50 = 62 nM
2 IC50 = 75 nM
CP0963886
2-[[4-[4-(5-fluoro-2-methoxy-phenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]cyclohex-3-en-1-yl]amino]acetic acid
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C22H22FN3O3
 1
1 IC50 = 63 nM
CP0773151
(1s,4s)-4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H28FN3O3
 1
1 IC50 = 64 nM
CP0546230
2-[4-[4-(1-cyclobutyl-6-oxopyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]-N,N-dimethylacetamide
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C25H31N5O2
 1
1 IC50 = 70 nM
CP0128822
US9073922, 288
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C27H30FN3O3
 2
1 IC50 = 71 nM
2 IC50 = 80 nM
CP0565903
US9073922, 241
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C25H28FN3O3
 2
1 IC50 = 80 nM
2 IC50 = 91 nM
CP0965399
(1s,4s)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H27F2N3O3
 1
1 IC50 = 81 nM
CP0914334
(1r,4r)-4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexanecarboxylic acid
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C26H28FN3O3
 1
1 IC50 = 83 nM
CP0579077
1-[4-[4-(4-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]ethanone
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C21H22FN3O2
 1
1 IC50 = 84 nM
CP0965400
2-((1s,4s)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexyl)acetic acid
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C27H30FN3O3
 1
1 IC50 = 86 nM
CP0961574
4-[4-(5-fluoro-2-methoxy-phenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-N-methylsulfonyl-cyclohex-3-ene-1-carboxamide
   Show/Hide
C22H22FN3O4S
 1
1 IC50 = 89 nM
CP0962478
1-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperidine-4-carboxylic acid
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C27H29F2N3O3
 1
1 IC50 = 100 nM
CP0537692
CHEMBL5209369
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C22H24FN3O2
 1
1 IC50 = 100 nM
CP0578436
(4-{4-[4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-3,6-dihydropyridin-1(2H)-yl}piperidin-1-yl)acetic acid
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C26H29FN4O3
 1
1 IC50 = 110 nM
CP0962662
2-(1-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperidin-4-yl)acetic acid
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C26H28FN3O3
 1
1 IC50 = 120 nM
CP0968689
2-((1r,4r)-4-(4-(5-fluoro-4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dihydropyridin-1(2H)-yl)cyclohexyl)acetic acid
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C27H29F2N3O3
 1
1 IC50 = 120 nM
CP0968691
2-(4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperazin-1-yl)acetic acid
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C26H29FN4O3
 1
1 IC50 = 130 nM
CP0572891
2-[4-[4-[1-(2-methoxyethyl)-6-oxopyridin-3-yl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]-N,N-dimethylacetamide
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C24H31N5O3
 1
1 IC50 = 130 nM
CP0968690
2-(4-(4-(4-(5-fluoro-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)cyclohex-3-enyl)piperidin-1-yl)acetic acid
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C27H30FN3O3
 1
1 IC50 = 160 nM
CP0577482
5-[2-[1-(2,2-difluoroethyl)piperidin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-propan-2-ylpyridin-2-one
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C22H26F2N4O
 1
1 IC50 = 160 nM
CP0545202
N,N-dimethyl-2-[4-[4-[1-(2-methylpropyl)-6-oxopyridin-3-yl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C25H33N5O2
 1
1 IC50 = 260 nM
CP0545201
2-[4-[4-(1-ethyl-6-oxopyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]-N,N-dimethylacetamide
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C23H29N5O2
 1
1 IC50 = 330 nM
CP0575772
4-(4-fluoro-2-methoxyphenyl)-2-(oxan-4-yl)-1H-pyrrolo[2,3-b]pyridine
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C19H19FN2O2
 1
1 IC50 = 400 nM
CP0577665
N,N-dimethyl-2-[4-[4-[1-(oxan-4-yl)-6-oxopyridin-3-yl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C26H33N5O3
 1
1 IC50 = 1200 nM
CP0554046
N,N-dimethyl-2-[4-[4-[1-(oxan-4-ylmethyl)-6-oxopyridin-3-yl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C27H35N5O3
 1
1 IC50 = 4000 nM
CP0577481
N,N-dimethyl-2-[4-[4-[1-[2-(oxan-4-yl)ethyl]-6-oxopyridin-3-yl]-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]acetamide
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C28H37N5O3
 1
1 IC50 = 4500 nM
CP0579078
2-[4-[4-(4-methoxy-1-methyl-6-oxopyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-2-yl]piperidin-1-yl]-N,N-dimethylacetamide
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C23H29N5O3
 1
1 IC50 = 30000 nM
Clinical Information about the Protein
Target 1 ( Cyclin-dependent kinase 9 (CDK9) )
Target Type Clinical trial Target
Disease 8 Target-related Diseases  8
1 Mantle cell lymphoma [ICD-11: 2A85.5]
2 Haematological malignancy [ICD-11: 2B33.Y]
3 Lymphoma [ICD-11: 2A80-2A86]
4 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
5 Non-hodgkin lymphoma [ICD-11: 2B33.5]
6 Acute myeloid leukaemia [ICD-11: 2A60]
7 Acute lymphoblastic leukaemia [ICD-11: 2A85]
8 Small-cell lung cancer [ICD-11: 2C25.Y]
Clinical Trial Drug(s) 7 Clinical Trial Drugs  7
1 P276-00 Phase 2
Mantle cell lymphoma
2 AZD4573 Phase 1
Haematological malignancy
3 CYC065 Phase 1
Lymphoma
4 SNS-032 Phase 1
Solid tumour/cancer
5 TP-1287 Phase 1
Solid tumour/cancer
6 VIP-152 Phase 1
Non-hodgkin lymphoma
7 Flavopiridol Phase 2
Acute myeloid leukaemia
Discontinued Drug(s) 2 Discontinued Drugs  2
1 SCH 727965 Discontinued in Phase 3
Acute lymphoblastic leukaemia
2 BAY 10-00394 Discontinued in Phase 2
Small-cell lung cancer