zotiraciclib [Ligand Id: 9095] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1944698 (TG02, SB-1317, SB1317, EX45, Zotiraciclib, Tg-02, Tg02)
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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 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 6/Cyclin-dependent kinase 6 in Human [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
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  • Janus kinase 1 in Human [GtoPdb: 2047] [UniProtKB: P23458]
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  • tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 3/CDK3/Cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038471] [GtoPdb: 1975] [UniProtKB: P24864Q00526]
ChEMBL Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate B 8.1 pIC50 8 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
GtoPdb - - 8.1 pIC50 8 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of recombinant human full length C-terminal His6-tagged CDK3/N-terminal GST-tagged cyclin E expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate B 8.52 pIC50 3 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 recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as substrate B 7.43 pIC50 37 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
ChEMBL Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 9/CDK9/Cyclin K in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038475] [GtoPdb: 1981] [UniProtKB: O75909P50750]
GtoPdb - - 8.52 pIC50 3 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of human recombinant full length His-tagged CDK9/cyclin K expressed in baculovirus expression system B 8.52 pIC50 3 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
GtoPdb - - 8.05 pIC50 9 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of CDK1 (unknown origin) B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
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 full-length His-tagged CDK1/cyclin B1 expressed in baculovirus expression system B 8.05 pIC50 9 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
GtoPdb - - 8.05 pIC50 9 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis B 6.89 pIC50 130 nM IC50 J. Med. Chem. (2012) 55: 169-196 [PMID:22148278]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2012) 55: 169-96 [PMID:22148278];
Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of CDK2 (unknown origin) B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of recombinant Cdk2/cyclin A using RbING as substrate after 2 hrs by luminescence assay B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2012) 55: 169-196 [PMID:22148278]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2012) 55: 169-96 [PMID:22148278];
Leukemia (2012) 26: 236-43 [PMID:21860433]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2012) 55: 169-96 [PMID:22148278];
Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of human recombinant GST-tagged CDK2/cyclin E1 B 8.3 pIC50 5 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
GtoPdb - - 8.4 pIC50 4 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of human GST-tagged CDK5 B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
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 human recombinant full-length GST/His-tagged CDK5/p25 expressed in baculovirus expression system by Z'-Lyte assay B 8.4 pIC50 4 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
GtoPdb - - 8.4 pIC50 4 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
ChEMBL Inhibition of human CDK6 B 7 pIC50 >100 nM IC50 J Med Chem (2019) 62: 4233-4251 [PMID:30543440]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
GtoPdb - - 8.52 pIC50 3 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
ChEMBL Inhibition of human GST-tagged CDK9 B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader B 6.77 pIC50 170 nM IC50 Eur. J. Med. Chem. (2015) 95: 104-115 [PMID:25800646]
ChEMBL Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay B 7.14 pIC50 73 nM IC50 J. Med. Chem. (2012) 55: 169-196 [PMID:22148278]
ChEMBL Inhibition of human recombinant GST-tagged JAK2 expressed in baculovirus expression system B 7.14 pIC50 73 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
GtoPdb - - 7.72 pIC50 19 nM IC50 J Med Chem (2012) 55: 169-96 [PMID:22148278];
Leukemia (2012) 26: 236-43 [PMID:21860433]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of recombinant Flt3 using poly(Glu,Tyr) as substrate after 2 hrs by luminescence assay B 7.25 pIC50 56 nM IC50 J. Med. Chem. (2012) 55: 169-196 [PMID:22148278]
ChEMBL Inhibition of human recombinant FLT3 after 1 hr by LanthaScreen assay platform B 7.38 pIC50 42 nM IC50 Eur. J. Med. Chem. (2015) 95: 104-115 [PMID:25800646]
ChEMBL Inhibition of human recombinant N-terminal GST-tagged FLT3 D835Y mutant expressed in baculovirus infected Sf21 insect cells using abltide as substrate B 7.68 pIC50 21 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
GtoPdb - - 7.72 pIC50 19 nM IC50 J Med Chem (2012) 55: 169-96 [PMID:22148278];
Leukemia (2012) 26: 236-43 [PMID:21860433]
colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 7.57 pIC50 27 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
Janus kinase 1 in Human [GtoPdb: 2047] [UniProtKB: P23458]
GtoPdb - - 7.23 pIC50 59 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]
tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597]
GtoPdb - - 7.85 pIC50 14 nM IC50 Leukemia (2012) 26: 236-43 [PMID:21860433]

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]