NS-49 [Ligand Id: 481] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL72958 (NS-49) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes | B | 5.95 | pKi | 1122.02 | nM | Ki | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
| GtoPdb | - | - | 6.2 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417] |
| ChEMBL | Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway | F | 6.5 | pEC50 | 316.23 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 471-475 [PMID:11814822] |
| ChEMBL | Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor | F | 6.8 | pEC50 | 158.49 | nM | EC50 | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Affinity to human Alpha-1B adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes | B | 4.95 | pKi | 11220.18 | nM | Ki | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
| GtoPdb | - | - | 5.1 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417] |
| ChEMBL | Activation of recombinant human adrenergic, alpha-1B receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway | F | 4 | pEC50 | <100000 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 471-475 [PMID:11814822] |
| ChEMBL | Agonist potency at Alpha-1B adrenergic receptor expressed in rat-1 fibroblasts | F | 4 | pEC50 | <100000 | nM | EC50 | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 327-34 [PMID:8719417] |
| ChEMBL | Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway | F | 4 | pEC50 | <100000 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 471-475 [PMID:11814822] |
| ChEMBL | Agonist potency at Alpha-1D adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1D adrenergic receptor | F | 4 | pEC50 | <100000 | nM | EC50 | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Agonist potency at Alpha-2A stably expressed in CHO cells. | F | 5 | pEC50 | <10000 | nM | EC50 | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Agonist potency at Alpha-2C adrenergic receptor assayed in CHO cells expressing human Alpha-2C adrenergic receptor | F | 5.7 | pEC50 | 1995.26 | nM | EC50 | J Med Chem (2002) 45: 2229-2239 [PMID:12014961] |
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]
