ML252 [Ligand Id: 14112] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2164048 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] | ||||||||
| ChEMBL | Antagonist activity at KCNQ1/E1 expressed in CHO cells incubated for 3 mins by automated patch clamp assay | F | 5.09 | pIC50 | 8120 | nM | IC50 | J Med Chem (2012) 55: 6975-6979 [PMID:22793372] |
| GtoPdb | Inhibitor activity at KCNQ1 channels expressed in CHO cells in a patch clamp assay | - | 5.53 | pIC50 | 2920 | nM | IC50 | Brain Res (1998) 808: 174-81 [PMID:9767160] |
| Kv7.3/Kv7.2/Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221348] [GtoPdb: 562, 561] [UniProtKB: O43525, O43526] | ||||||||
| ChEMBL | Antagonist activity at KCNQ2/Q3 expressed in CHO cells incubated for 3 mins by automated patch clamp assay | F | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2012) 55: 6975-6979 [PMID:22793372] |
| GtoPdb | Inhibitor activity at KCNQ2 channels expressed in CHO cells in a patch clamp assay | - | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2012) 55: 6975-9 [PMID:22793372] |
| Kv7.1/Voltage-gated potassium channel subunit Kv7.1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1866] [GtoPdb: 560] [UniProtKB: P51787] | ||||||||
| GtoPdb | Inhibitor activity at KCNQ1 channels expressed in CHO cells in a patch clamp assay | - | 5.53 | pIC50 | 2920 | nM | IC50 | Brain Res (1998) 808: 174-81 [PMID:9767160] |
| ChEMBL | Antagonist activity at KCNQ1 expressed in CHO cells incubated for 3 mins by automated patch clamp assay | F | 5.53 | pIC50 | 2920 | nM | IC50 | J Med Chem (2012) 55: 6975-6979 [PMID:22793372] |
| Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526] | ||||||||
| GtoPdb | Inhibitor activity at KCNQ2 channels expressed in CHO cells in a patch clamp assay | - | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2012) 55: 6975-9 [PMID:22793372] |
| ChEMBL | Antagonist activity at KCNQ2 expressed in CHO cells incubated for 3 mins by automated patch clamp assay | F | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2012) 55: 6975-6979 [PMID:22793372] |
| Kv7.4/Voltage-gated potassium channel subunit Kv7.4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3576] [GtoPdb: 563] [UniProtKB: P56696] | ||||||||
| ChEMBL | Antagonist activity at KCNQ4 expressed in CHO cells incubated for 3 mins by automated patch clamp assay | F | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2012) 55: 6975-6979 [PMID:22793372] |
| GtoPdb | Inhibitor activity at KCNQ4 channels expressed in CHO cells in a patch clamp assay | - | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2012) 55: 6975-9 [PMID:22793372] |
ChEMBL data shown on this page come from version 35:
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]
