dilazep [Ligand Id: 4717] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL126075 (Dilazep, Dilazep dihydrochloride) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Equilibrative nucleoside transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808] | ||||||||
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | |
| ChEMBL | Inhibition of human ENT1 expressed in porcine PK15NTD cells by cell-based [3H]5-uridine uptake assay | B | 7.76 | pIC50 | 17.5 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5801-5804 [PMID:25454272] |
| ChEMBL | Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay (PubChem AID: 1745861) | F | 10 | pIC50 | 0.1 | nM | IC50 | Sci Rep (2019) 9: 13802-null [PMID:31551431] |
| Equilibrative nucleoside transporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287614] [GtoPdb: 1118] [UniProtKB: O54699] | ||||||||
| ChEMBL | Inhibition of rat ENT2 expressed in rat H9c2 cells by cell-based 3H[5-]uridine uptake assay | B | 5.06 | pIC50 | 8800 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5801-5804 [PMID:25454272] |
| ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells | F | 4.7 | pIC50 | 20000 | nM | IC50 | Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538] |
| ABCC5/Multidrug resistance-associated protein 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538] |
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]
