atuveciclib [Ligand Id: 11687] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4439321 (Atuveciclib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| calcium/calmodulin-dependent protein kinase II beta subunit/CaM kinase II beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CAMK2B | B | 5.78 | pIC50 | 1650 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CAMK2D | B | 5.48 | pIC50 | 3340 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| calcium/calmodulin-dependent protein kinase II gamma subunit/CaM kinase II gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CAMK2G | B | 5.68 | pIC50 | 2081 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 3/CDK3/Cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038471] [GtoPdb: 1975] [UniProtKB: P24864, Q00526] | ||||||||
| ChEMBL | Inhibition of C-terminal His6-tagged human CDK3/N-terminal GST-tagged human cyclin E expressed in baculovirus infected Sf21 insect cells | B | 6.05 | pIC50 | >890 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CDK6 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of N-terminal His6-tagged human CDK6/N-terminal GST-tagged human cyclin D3 expressed in baculovirus infected Sf21 insect cells | B | 6.05 | pIC50 | >890 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CDK7 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of full length human CDK7/C-terminal His6-tagged human cyclin H/N-terminal GST-tagged human MAT1 expressed in baculovirus infected Sf21 insect cells | B | 6.05 | pIC50 | >890 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 9/CDK9/Cyclin K in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038475] [GtoPdb: 1981] [UniProtKB: O75909, P50750] | ||||||||
| GtoPdb | Inhibition of CDK9/CycT1 in vitro, at physiological (high) ATP concentration | - | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2021) 64: 11651-11674 [PMID:34264057] |
| ChEMBL | Selectivity interaction (NanoBRET assay in HEK293T cells) EUB0001631a CDK9 | B | 6.82 | pIC50 | 150 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | Inhibition of CDK9/CycT1 in vitro, at low ATP concentration | - | 7.89 | pIC50 | 13 | nM | IC50 | ChemMedChem (2017) 12: 1776-1793 [PMID:28961375] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| GtoPdb | Inhibition of CDK9/CycT1 in vitro, at physiological (high) ATP concentration | - | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2021) 64: 11651-11674 [PMID:34264057] |
| ChEMBL | Competitive reversible inhibition of recombinant full-length His-tagged human CDK9/cyclin T expressed in baculovirus infected insect cells using biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed b substrate addition measured after 25 mins in presence of high ATP by TR-FRET analysis | B | 6.42 | pIC50 | 380 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Competitive reversible inhibition of recombinant full-length His-tagged human CDK9/cyclin T expressed in baculovirus infected insect cells using biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed b substrate addition measured after 25 mins in presence of low ATP by TR-FRET analysis | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK9/cyclin T (unknown origin) using YSPTSPSYSPTSPSYSPTSPKKK or histone H1 as substrate incubated for 2 hrs in presence of [gamma-33P]ATP by radioactive filter binding assay | B | 7.88 | pIC50 | 13.1 | nM | IC50 | Eur J Med Chem (2021) 211: 113091-113091 [PMID:33338869] |
| ChEMBL | Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed by ATP and substrate addition and measured after 25 mins by TR-FRET assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2020) 63: 14243-14275 [PMID:32870008] |
| ChEMBL | Inhibition of His-tagged full-length recombinant human CDK9/Cyclin T1 expressed in insect cells using Biotin-tagged Ttds-YISPLKSPYKISEG peptide as substrate incubated for 15 mins by TR-FRET assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2022) 65: 6390-6418 [PMID:35485642] |
| ChEMBL | Affinity Biochemical interaction: (TR-FRET assay (inhibition of CDK9/cyclinT1 phosphorylation using 10 uM ATP)) EUB0001631a CDK9 | B | 7.89 | pIC50 | 13 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | Inhibition of CDK9/CycT1 in vitro, at low ATP concentration | - | 7.89 | pIC50 | 13 | nM | IC50 | ChemMedChem (2017) 12: 1776-1793 [PMID:28961375] |
| ChEMBL | Inhibition of C-terminal His6-tagged human CDK9/cyclin-T1 expressed in baculovirus infected Sf21 insect cells | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CDK9 | B | 8.22 | pIC50 | 6 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CDK1 | B | 5.96 | pIC50 | 1100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of N-terminal GST-tagged thrombin cleavage site-fused human CDK1/cyclin-B expressed in baculovirus infected Sf9 insect cells | B | 6.05 | pIC50 | >890 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of CDK2 (unknown origin) | B | 6.33 | pIC50 | 470 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] | ||||||||
| ChEMBL | Selectivity interaction (TR-FRET assay) EUB0001631a CDK2 | B | 4.89 | pIC50 | >13000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CDK2 | B | 6 | pIC50 | 1000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in sf9 cells using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed by ATP and substrate addition and measured after 25 mins by TR-FRET assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2020) 63: 14243-14275 [PMID:32870008] |
| ChEMBL | Inhibition of C-terminal His6-tagged human CDK2/N-terminal GST-tagged human cyclin E expressed in baculovirus infected Sf21 insect cells | B | 6.05 | pIC50 | >890 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| 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 | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a CDK5 | B | 5.8 | pIC50 | 1600 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of N-terminal GST-tagged human CDK5/N-terminal GST-tagged p35 | B | 6.05 | pIC50 | >890 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTitre-Glo Luminescent Cell Viability Assay (Promega, HeLa cells)) EUB0001631a CDK9 | F | 6.04 | pIC50 | 920 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of CDK9 (unknown origin) | B | 6.41 | pIC50 | 385 | nM | IC50 | Eur J Med Chem (2017) 142: 424-458 [PMID:28911822] |
| GtoPdb | Inhibition of CDK9/CycT1 in vitro, at physiological (high) ATP concentration | - | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2021) 64: 11651-11674 [PMID:34264057] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTitre-Glo Luminescent Cell Viability Assay (Promega using MOLM-13 cells)) EUB0001631a CDK9 | F | 6.51 | pIC50 | 310 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | Inhibition of CDK9/CycT1 in vitro, at low ATP concentration | - | 7.89 | pIC50 | 13 | nM | IC50 | ChemMedChem (2017) 12: 1776-1793 [PMID:28961375] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a EPHA1 | B | 5.76 | pIC50 | 1737 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a EPHB1 | B | 5.69 | pIC50 | 2032 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Inhibition of human GSK3alpha | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a GSK3A | B | 7.35 | pIC50 | 45 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of human GSK3beta | B | 7.06 | pIC50 | 87 | nM | IC50 | J Med Chem (2020) 63: 13228-13257 [PMID:32866383] |
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a GSK3B | B | 7.06 | pIC50 | 87 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a IRAK1 | B | 5.26 | pIC50 | 5454 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a MAP3K9 | B | 5.52 | pIC50 | 3010 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a ABL2 | B | 5.55 | pIC50 | 2843 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a FGR | B | 5.11 | pIC50 | 7754 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a LYN | B | 5.45 | pIC50 | 3514 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a SRC | B | 5.28 | pIC50 | 5293 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Selectivity interaction (Merck Millipore (enzymatic assay) ) EUB0001631a YES1 | B | 5.83 | pIC50 | 1495 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
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]
