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ChEMBL ligand: CHEMBL1234833 |
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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 kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
ChEMBL | Inhibition of CAMKKbeta | B | 5.61 | pIC50 | 2450 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
ChEMBL | Inhibition of CK1 | B | 5.98 | pIC50 | 1040 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
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 assessed as amount of ATP released by luciferase activity based PKLight assay | B | 4.45 | pIC50 | 35500 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
ChEMBL | Inhibition of CDK9/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
GtoPdb | - | - | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
cyclin dependent kinase 8/Cell division protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336] | ||||||||
ChEMBL | Competitive reversible inhibition of CDK8 (unknown origin) | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
GtoPdb | - | - | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Inhibition of CDK1/cyclinB1 assessed as amount of ATP released by luciferase activity based PKLight assay | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Competitive reversible inhibition of CDK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
ChEMBL | Inhibition of human CDK2 expressed in baculovirus infected Sf9 cells using Histone H1 as substrate incubated for 10 mins by scintillation counting method | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2021) 218: 113389-113389 [PMID:33784602] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Inhibition of CDK2/cyclinE assessed as amount of ATP released by luciferase activity based PKLight assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
ChEMBL | Competitive reversible inhibition of CDK4 (unknown origin) | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
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 CDK4/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Competitive reversible inhibition of CDK5 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
ChEMBL | Competitive reversible inhibition of CDK6 (unknown origin) | B | 4.45 | pIC50 | 35500 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
GtoPdb | - | - | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Competitive reversible inhibition of CDK7 (unknown origin) | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613, P51946] | ||||||||
GtoPdb | - | - | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Inhibition of CDK7/cyclinH/MAT1 assessed as amount of ATP released by luciferase activity based PKLight assay | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
cyclin dependent kinase 5/Cyclin-T1/Cyclin-dependent-like kinase 5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885549] [GtoPdb: 1977] [UniProtKB: O60563, Q00535] | ||||||||
GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Inhibition of CDK5/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
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 DYRK1A | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
Insulin receptor-related receptor/Insulin receptor-related protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5483] [GtoPdb: 1802] [UniProtKB: P14616] | ||||||||
ChEMBL | Inhibition of IRR | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
ChEMBL | Inhibition of ERK1 | B | 5.43 | pIC50 | 3730 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
ChEMBL | Inhibition of ERK2 | B | 5.51 | pIC50 | 3110 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08] | ||||||||
GtoPdb | - | - | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2010) 53: 8508-22 [PMID:21080703] |
ChEMBL | Inhibition of ERK8 | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
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]