asnuciclib [Ligand Id: 12074] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2347597 (Asnuciclib, CDKI-73, CDKI73)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of human recombinant His6 tagged CDK9/CyclinT1 expressed in Sf21 insect cells after 40 mins by scintillation counting analysis B 8.4 pKi 4 nM Ki J Med Chem (2013) 56: 640-659 [PMID:23301767]
ChEMBL Inhibition of CDK9/cyclin T1 (unknown origin) assessed as inhibition constant B 8.4 pKi 4 nM Ki Bioorg Med Chem (2023) 80: 117158-117158 [PMID:36706608]
ChEMBL Inhibition of CDK9/cyclin T1 (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis B 8.4 pKi 4 nM Ki Bioorg Med Chem (2023) 80: 117158-117158 [PMID:36706608]
GtoPdb inhibition of CDK9/CyclinT1 expressed in Sf21 insect cells - 8.4 pKi 4 nM Ki J Med Chem (2013) 56: 640-59 [PMID:23301767]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
ChEMBL Inhibition of CDK1/Cyclin B (unknown origin) assessed as inhibition constant B 8.4 pKi 4 nM Ki Bioorg Med Chem (2023) 80: 117158-117158 [PMID:36706608]
ChEMBL Inhibition of CDK1/Cyclin B (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis B 8.4 pKi 4 nM Ki Bioorg Med Chem (2023) 80: 117158-117158 [PMID:36706608]
GtoPdb Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells - 8.4 pKi 4 nM Ki J Med Chem (2013) 56: 640-59 [PMID:23301767]
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 human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells after 40 mins by scintillation counting analysis B 8.4 pKi 4 nM Ki J Med Chem (2013) 56: 640-659 [PMID:23301767]
GtoPdb Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells - 8.4 pKi 4 nM Ki J Med Chem (2013) 56: 640-59 [PMID:23301767]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
GtoPdb Inhibition of human recombinant His6 tagged CDK2/Cyclin A expressed in Sf21 insect cells - 8.52 pKi 3 nM Ki J Med Chem (2013) 56: 640-59 [PMID:23301767]
ChEMBL Inhibition of human recombinant His6 tagged CDK2/Cyclin A expressed in Sf21 insect cells after 40 mins by scintillation counting analysis B 8.52 pKi 3 nM Ki J Med Chem (2013) 56: 640-659 [PMID:23301767]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020P24864P24941]
GtoPdb Inhibition of human recombinant His6 tagged CDK2/Cyclin A expressed in Sf21 insect cells - 8.52 pKi 3 nM Ki J Med Chem (2013) 56: 640-59 [PMID:23301767]
ChEMBL Inhibition of CDK2/cyclin E (unknown origin) assessed as inhibition constant B 8.52 pKi 3 nM Ki Bioorg Med Chem (2023) 80: 117158-117158 [PMID:36706608]
ChEMBL Inhibition of CDK2/cyclin E (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis B 8.52 pKi 3 nM Ki Bioorg Med Chem (2023) 80: 117158-117158 [PMID:36706608]
cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613P51946]
GtoPdb Inhibuition of CDK7/CyclinH/MAT1 expressed in Sf21 insect cells - 7.04 pKi 91 nM Ki J Med Chem (2013) 56: 640-59 [PMID:23301767]
ChEMBL Inhibition of human recombinant His6 tagged CDK7/CyclinH/MAT1 expressed in Sf21 insect cells after 40 mins by scintillation counting analysis B 7.04 pKi 91 nM Ki J Med Chem (2013) 56: 640-659 [PMID:23301767]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]