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ChEMBL ligand: CHEMBL3301610 (Ly-2835219, LY2835219, Abemaciclib, LY-2835219, Verzenios, Verzenio) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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calcium/calmodulin dependent protein kinase I/CaM kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2493] [GtoPdb: 1952] [UniProtKB: Q14012] | ||||||||
ChEMBL | Inhibition of wild-type human full length CAMK1A (M1 to L370 residues) expressed in bacterial expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | B | 8 | pKi | <10 | nM | Ki | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged CDK2 (1 to 298 residues)/cyclin A2 (1 to 432 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE ultra kinase assay | B | 7.32 | pIC50 | 47.6 | nM | IC50 | Eur J Med Chem (2019) 178: 352-364 [PMID:31200237] |
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 | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
cyclin dependent kinase 4/CDK4/Cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038472] [GtoPdb: 1976] [UniProtKB: P11802, P30281] | ||||||||
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged CDK4 (1 to 303 residues)/cyclin D3 (1 to 292 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE ultra kinase assay | B | 8.74 | pIC50 | 1.82 | nM | IC50 | Eur J Med Chem (2019) 178: 352-364 [PMID:31200237] |
cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385, Q00534] | ||||||||
ChEMBL | Inhibition of recombinant full length human N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation counting analysis | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
GtoPdb | CDK6/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8 | pIC50 | 10 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged CDK4 (M1 to A326 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534] | ||||||||
ChEMBL | Competitive inhibition of CDK6/cyclin D3 (unknown origin) assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP | B | 8.09 | pKi | 8.2 | nM | Ki | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
GtoPdb | CDK6/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8 | pIC50 | 10 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of human CDK6/Cyclin-D3 | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2018) 148: 140-153 [PMID:29459274] |
ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D3 (1 to 292 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE ultra kinase assay | B | 8.14 | pIC50 | 7.27 | nM | IC50 | Eur J Med Chem (2019) 178: 352-364 [PMID:31200237] |
ChEMBL | Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
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 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 | 5.41 | pKi | 3910 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | B | 5.51 | pIC50 | 3112 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 | 5.51 | pIC50 | 3100 | 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 CDK9/cyclin T (unknown origin) | B | 7.24 | pKi | 57 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Inhibition of CDK9/Cyclin T1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | B | 7 | pIC50 | 101 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 | 7 | pIC50 | 101 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
ChEMBL | Inhibition of human CDK9/Cyclin-T1 | B | 7.24 | pIC50 | 57 | nM | IC50 | Eur J Med Chem (2018) 148: 140-153 [PMID:29459274] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
ChEMBL | Inhibition of CDK1 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | B | 5.82 | pIC50 | 1523 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5332-5336 [PMID:29074254] |
ChEMBL | Inhibition of CDK1 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
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 CDK1/cyclin B (unknown origin) | B | 5.79 | pKi | 1627 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Inhibition of human CDK1/cyclin B1 (unknown origin) | B | 5.79 | pIC50 | 1627 | nM | IC50 | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
ChEMBL | Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP | B | 6.43 | pIC50 | 371 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 | 6.43 | pIC50 | 371 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
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 | 6.3 | pIC50 | >500 | nM | IC50 | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
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 human CDK2/cyclin E | B | 6.3 | pKi | 504 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
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 | 6.46 | pIC50 | 347 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
ChEMBL | Inhibition of CDK4 (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2017) 142: 424-458 [PMID:28911822] |
ChEMBL | Inhibition of CDK4 (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of CDK4 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5332-5336 [PMID:29074254] |
ChEMBL | Inhibition of CDK4 (unknown origin) after 90 mins by ADP-Glo assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
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 recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation counting analysis | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Competitive inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
ChEMBL | Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATP | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
ChEMBL | Inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by microplate scintillation counter | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4/G1/S-specific cyclin-E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885554] [GtoPdb: 1976] [UniProtKB: P11802, P24864] | ||||||||
ChEMBL | Inhibition of human CDK4/cyclin D1 using ULight-substrate after 1 hr by LANCE assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2018) 148: 140-153 [PMID:29459274] |
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
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 CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATP | B | 6.39 | pIC50 | 405 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 | 6.39 | pIC50 | 405 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
GtoPdb | CDK6/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8 | pIC50 | 10 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of CDK6 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2017) 142: 424-458 [PMID:28911822] |
ChEMBL | Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
ChEMBL | Inhibition of CDK6 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
ChEMBL | Inhibition of CDK6 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5332-5336 [PMID:29074254] |
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
ChEMBL | Inhibition of CDK7 (unknown origin) | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
ChEMBL | Inhibition of CDK9 (unknown origin) | B | 7.24 | pIC50 | 57 | nM | IC50 | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
ChEMBL | Inhibition of wild-type human partial length DYRK1A (H129 to S509 residues) expressed in mammalian expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | B | 8 | pKi | <10 | nM | Ki | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 4.96 | pIC50 | 10900 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
homeodomain interacting protein kinase 1/Homeodomain-interacting protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5427] [GtoPdb: 2033] [UniProtKB: Q86Z02] | ||||||||
ChEMBL | Inhibition of wild-type human partial length HIPK1 (M146 to I555 residues) expressed in mammalian expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | B | 8 | pKi | <10 | nM | Ki | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
ChEMBL | Inhibition of wild-type human partial length PIM1 (A15 to K313 residues) expressed in bacterial expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | B | 8 | pKi | <10 | nM | Ki | Eur J Med Chem (2019) 172: 143-153 [PMID:30978559] |
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]