(R)-CR8 [Ligand Id: 11065] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL518800 |
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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 A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
| ChEMBL | Inhibition of GST-tagged CDK2/Cyclin-A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate measured in presence of [gamma-33P]ATP | B | 6.84 | pIC50 | 144 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| 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 N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-33P]ATP | B | 5.75 | pIC50 | 1769 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-33P]ATP | B | 6.57 | pIC50 | 272 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| 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 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP | B | 6.1 | pIC50 | 787 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| GtoPdb | Inhibition of CDK1/cyclin E complex in vitro. | - | 7.39 | pIC50 | 41 | nM | IC50 | Oncogene (2008) 27: 5797-807 [PMID:18574471] |
| 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 CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP | B | 7.21 | pIC50 | 62 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| ChEMBL | Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| 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-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP | B | 4.58 | pIC50 | 26090 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP | B | 6.65 | pIC50 | 225 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| GtoPdb | Inhibition of CDK5/p25 complex in vitro. | - | 6.96 | pIC50 | 110 | nM | IC50 | Oncogene (2008) 27: 5797-807 [PMID:18574471] |
| 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 recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP | B | 6.65 | pIC50 | 225 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| GtoPdb | Inhibition of CDK5/p25 complex in vitro. | - | 6.96 | pIC50 | 110 | nM | IC50 | Oncogene (2008) 27: 5797-807 [PMID:18574471] |
| Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7] | ||||||||
| ChEMBL | MERS_3CL Pro protease inhibition IC50 by FRET kind of response from peptide substrate | F | 5 | pIC50 | >10000 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate | F | 6.08 | pIC50 | 840 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
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]
