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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
