narazaciclib [Ligand Id: 11879] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3115681 (Narazaciclib, On123300, On-123300)
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
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  • NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
ChEMBL Inhibition of CDK2/cyclinA (unknown origin) B 6.8 pIC50 159 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
ChEMBL Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385, Q00534]
ChEMBL Inhibition of CDK6/cyclinD1 (unknown origin) B 8.01 pIC50 9.82 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
GtoPdb CDK6/CyclinD1 - 8.01 pIC50 9.82 nM IC50 J Med Chem (2014) 57: 578-99 [PMID:24417566]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948]
ChEMBL Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 5.22 pIC50 6000 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.93 pIC50 117 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
ChEMBL Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.22 pIC50 600 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.42 pIC50 377 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385]
ChEMBL Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.74 pIC50 18 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK2/CyclinD1 - 8.41 pIC50 3.9 nM IC50 J Med Chem (2014) 57: 578-99 [PMID:24417566]
ChEMBL Inhibition of CDK4/cyclinD1 (unknown origin) using retinoblastoma as substrate after 30 mins by autoradiography in presence of [gamma-32P]ATP B 8.41 pIC50 3.87 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
ChEMBL Inhibition of CDK4/cyclinD1 (unknown origin) B 8.42 pIC50 3.8 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.57 pIC50 272 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 (unknown origin) B 7.59 pIC50 26 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL Inhibition of FMS (unknown origin) B 8 pIC50 10 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
ChEMBL Inhibition of ARK5 (unknown origin) B 8.31 pIC50 4.95 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
GtoPdb - - 8.31 pIC50 4.95 nM IC50 J Med Chem (2014) 57: 578-99 [PMID:24417566]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 6.84 pIC50 144 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibition of PDGFRbeta (unknown origin) B 7.59 pIC50 26 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL (unknown origin) B 7.27 pIC50 53.32 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of FYN (unknown origin) B 7.96 pIC50 11.09 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
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 FLT3 (unknown origin) B 7.91 pIC50 12.22 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]