narazaciclib [Ligand Id: 11879] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3115681 (On-123300, On123300, Narazaciclib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/AMPK alpha1/beta2/gamma1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038453] [GtoPdb: 1544, 1545, 1541] [UniProtKB: O43741, P54619, Q13131] | ||||||||
| ChEMBL | Inhibition of AMPKA alpha1/beta2/gamma1(unknown origin) using sakamototide peptide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 5.9 | pIC50 | 1258.93 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| cyclin dependent kinase 2/CDK2/Cyclin A2 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 B1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961, 3352] [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 regulatory subunit 1/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977, 3344] [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] |
| ChEMBL | Inhibition of FGFR1 (unknown origin) | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 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] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Inhibition of MARK3 (unknown origin) using CHKTide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 5.8 | pIC50 | 1584.89 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] | ||||||||
| ChEMBL | Inhibition of MARK4 (unknown origin) using CHKTide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 5 | pIC50 | 10000 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
| ChEMBL | Binding affinity to NanoLuc fused-NUAK1 (unknown origin) transfected in HEK293 cells assessed as target engagement incubated for 90 mins in presence of K5 tracer using NanoGlo as substrate by Nano BRET assay | B | 6 | pIC50 | 1000 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| ChEMBL | Inhibition of NUAK1 (unknown origin) using sakamototide peptide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 7.6 | pIC50 | 25.12 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| ChEMBL | Inhibition of ARK5 (unknown origin) | B | 8.31 | pIC50 | 4.95 | nM | IC50 | J Med Chem (2014) 57: 578-599 [PMID:24417566] |
| ChEMBL | Inhibition of human NUAK1 | B | 8.31 | pIC50 | 4.95 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| GtoPdb | - | - | 8.31 | pIC50 | 4.95 | nM | IC50 | J Med Chem (2014) 57: 578-99 [PMID:24417566] |
| NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093] | ||||||||
| ChEMBL | Inhibition of NUAK2 (unknown origin) using sakamototide peptide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 8.3 | pIC50 | 5.01 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 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] |
| ChEMBL | Inhibition of PDGFRb (unknown origin) | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of RET (unknown origin) | B | 8.04 | pIC50 | 9.2 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase 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] |
| microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2] | ||||||||
| ChEMBL | Inhibition of MARK1 (unknown origin) using CHKTide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 5.2 | pIC50 | 6309.57 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Inhibition of MARK2 (unknown origin) using CHKTide as substrate in presence of ATP preincubated for 60 mins followed by substrate and ATP addition and measured after 40 mins by ADP-Glo kinase assay | B | 4.8 | pIC50 | 15848.93 | nM | IC50 | ACS Med Chem Lett (2025) 16: 327-335 [PMID:39967649] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 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] |
| ChEMBL | Inhibition of FYN (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
ChEMBL data shown on this page come from version 37:
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]
