dinaciclib [Ligand Id: 7379] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2103840 (Dinaciclib, SCH-727965, Mk-7965, SCH 727965)
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Inhibition of N-terminal 6His-tagged human BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay B 4.72 pIC50 19000 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL Inhibition of N-terminal 6His-tagged human BRDT bromodomain 1 (21 to 137 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay B 4.43 pIC50 37000 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248P24941]
ChEMBL Inhibition of GST-tagged CDK2/Cyclin-A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate measured in presence of [gamma-33P]ATP B 8.52 pIC50 3 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
GtoPdb Inhibition of CDK2/cyclin E complex. - 8.7 pIC50 2 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
GtoPdb - - 9 pIC50 1 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
ChEMBL Inhibition of recombinant CDK2/cyclin A (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis B 9 pIC50 1 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613P51946P51948]
ChEMBL Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP B 6.77 pIC50 170 nM IC50 Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853]
ChEMBL Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-33P]ATP B 6.77 pIC50 170 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of CDK9/Cyclin T1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP B 6.75 pIC50 178 nM IC50 Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853]
ChEMBL Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-33P]ATP B 7.82 pIC50 15 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
ChEMBL Inhibition of recombinant CDK9/cyclin T (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis B 8.4 pIC50 4 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of recombinant full-length N-terminal GST-tagged human CDK9 (1 to 372 residues)/full-length His6-tagged human cyclin T1 (1 to 726 residues) expressed in baculovirus expression system using 5'FAM-RRRFRPASPLRGPPK-COOH as substrate after 30 mins by microfluidic assay B 8.4 pIC50 4 nM IC50 MedChemComm (2016) 7: 1580-1586
ChEMBL Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal GST-HIS6 fusion protein tagged human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells at 10 uM using TAMRA-Rbtide substrate and ATP incubated for 1 hr by fluorescent polarization assay B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2018) 28: 769-773 [PMID:29329658]
GtoPdb - - 8.4 pIC50 4 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibition of CDK1 (unknown origin) B 7.14 pIC50 72 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
GtoPdb - - 8.52 pIC50 3 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
ChEMBL Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK1 (unknown origin) B 8.52 pIC50 3 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate after 1 hr by liquid scintillation counting analysis B 8.52 pIC50 3 nM IC50 Bioorg Med Chem (2018) 26: 3491-3501 [PMID:29853338]
ChEMBL Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method B 8.52 pIC50 3 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
ChEMBL Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method B 8.52 pIC50 3 nM IC50 Eur J Med Chem (2019) 172: 143-153 [PMID:30978559]
ChEMBL Inhibition of CDK1 (unknown origin) B 8.52 pIC50 3 nM IC50 Eur J Med Chem (2019) 183: 111641-111641 [PMID:31514062]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP B 7.14 pIC50 72 nM IC50 Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853]
ChEMBL Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP B 7.14 pIC50 72 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
GtoPdb - - 8.52 pIC50 3 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
ChEMBL Inhibition of recombinant CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
GtoPdb Inhibition of CDK2/cyclin E complex. - 8.7 pIC50 2 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
GtoPdb - - 9 pIC50 1 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
ChEMBL Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis B 9 pIC50 1 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK2 (unknown origin) B 9 pIC50 1 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate after 1 hr by liquid scintillation counting analysis B 9 pIC50 1 nM IC50 Bioorg Med Chem (2018) 26: 3491-3501 [PMID:29853338]
ChEMBL Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method B 9 pIC50 1 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
ChEMBL Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method B 9 pIC50 1 nM IC50 Eur J Med Chem (2019) 172: 143-153 [PMID:30978559]
ChEMBL Inhibition of CDK2 (unknown origin) B 9 pIC50 1 nM IC50 Eur J Med Chem (2019) 183: 111641-111641 [PMID:31514062]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
ChEMBL Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP B 8.7 pIC50 2 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
ChEMBL Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP B 8.7 pIC50 2 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
GtoPdb Inhibition of CDK2/cyclin E complex. - 8.7 pIC50 2 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
GtoPdb - - 9 pIC50 1 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibition of CDK4 (unknown origin) B 6.9 pIC50 127 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATP B 6.9 pIC50 127 nM IC50 Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853]
ChEMBL Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP B 6.94 pIC50 115 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP B 7.35 pIC50 45 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
GtoPdb - - 9 pIC50 1 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
ChEMBL Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis B 9 pIC50 1 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK5 (unknown origin) B 9 pIC50 1 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate after 1 hr by liquid scintillation counting analysis B 9 pIC50 1 nM IC50 Bioorg Med Chem (2018) 26: 3491-3501 [PMID:29853338]
ChEMBL Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method B 9 pIC50 1 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
ChEMBL Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method B 9 pIC50 1 nM IC50 Eur J Med Chem (2019) 172: 143-153 [PMID:30978559]
ChEMBL Inhibition of CDK5 (unknown origin) B 9 pIC50 1 nM IC50 Eur J Med Chem (2019) 183: 111641-111641 [PMID:31514062]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP B 7.17 pIC50 67 nM IC50 J Med Chem (2019) 62: 4606-4623 [PMID:30943029]
ChEMBL Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATP B 7.35 pIC50 45 nM IC50 Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853]
GtoPdb - - 9 pIC50 1 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
ChEMBL Inhibition of recombinant CDK5/p25 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis B 9 pIC50 1 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Inhibition of CDK9 (unknown origin) B 6.75 pIC50 178 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
ChEMBL Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1 hr in presence of 33P-ATP by liquid scintillation counting analysis B 8.4 pIC50 4 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK9 (unknown origin) B 8.4 pIC50 4 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate after 1 hr by liquid scintillation counting analysis B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2018) 26: 3491-3501 [PMID:29853338]
ChEMBL Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H1 as substrate incubated for 1 hr in presence of cyclin by [33P]-ATP-based liquid scintillation counting method B 8.4 pIC50 4 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
ChEMBL Inhibition of recombinant CDK9 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated peptide as substrate after 1 hr in presence of [33P]ATP by TopCount scintillation counting method B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2019) 172: 143-153 [PMID:30978559]
ChEMBL Inhibition of CDK9 (unknown origin) B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2019) 183: 111641-111641 [PMID:31514062]
GtoPdb - - 8.4 pIC50 4 nM IC50 ACS Chem Biol (2013) 8: 2360-5 [PMID:24007471]
Heat shock factor protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5869] [UniProtKB: Q00613]
ChEMBL Inhibition of 17AAG-induced HSF1-mediated HSP72 expression in human U2OS cells preincubated for 1 hr followed by 17AAG addition measured after 18 hrs by ELISA B 8.15 pIC50 7 nM IC50 MedChemComm (2016) 7: 1580-1586

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]