RS 100235 [Ligand Id: 250] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL69733 (RS-100235)
  • 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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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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  • 5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
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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 Compound was evaluated for binding affinity against Alpha-1C adrenergic receptor using radioligand binding assay B 6.5 pKi 316.23 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Compound was evaluated for binding affinity against Alpha-1B adrenergic receptor using radioligand binding assay B 6.3 pKi 501.19 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Compound was evaluated for binding affinity against Alpha-2A adrenergic receptor using radioligand binding assay B 7 pKi 100 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Compound was evaluated for binding affinity against Alpha-2B adrenergic receptor using radioligand binding assay B 5.6 pKi 2511.89 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
ChEMBL Compound was evaluated for binding affinity against Angiotensin II receptor, type 2 using radioligand binding assay B 5 pKi <10000 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Compound was evaluated for binding affinity against Dopamine D1 receptor using radioligand binding assay B 5 pKi <10000 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Compound was evaluated for binding affinity against Dopamine D2 receptor using radioligand binding assay B 6.5 pKi 316.23 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Compound was evaluated for binding affinity against Muscarinic M1 receptor using radioligand binding assay B 5.8 pKi 1584.89 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Compound was evaluated for binding affinity against Muscarinic M2 receptor using radioligand binding assay B 5.9 pKi 1258.93 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay B 5.7 pKi 1995.26 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL Compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor using radioligand binding assay B 6 pKi 1000 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Compound was evaluated for binding affinity against 5-hydroxytryptamine 2A receptor using radioligand binding assay B 6.3 pKi 501.19 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Compound was evaluated for binding affinity against 5-hydroxytryptamine 2C receptor using radioligand binding assay B 5.8 pKi 1584.89 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL Compound was evaluated for binding affinity against 5-hydroxytryptamine 3 receptor using radioligand binding assay B 6.3 pKi 501.19 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Compound was evaluated for binding affinity against 5-hydroxytryptamine 4 receptor using radioligand binding assay using [3H]GR as radioligand B 10 pKi 0.1 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Compound was evaluated for binding affinity against Angiotensin II receptor, type 1 using radioligand binding assay B 5 pKi <10000 nM Ki Bioorg Med Chem Lett (1995) 5: 2119-2122
5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
GtoPdb - - 12.2 pKi 0 nM Ki Neuroreport (1997) 8: 3189-96 [PMID:9351641];
Br J Pharmacol (2004) 143: 361-70 [PMID:15351779]

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]