NS-49 [Ligand Id: 481] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL72958 (NS-49)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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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 32:

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]