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 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]