Ro 60-0175 [Ligand Id: 166] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL76781 (Ro-60-0175, Ro-600175) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| ChEMBL | Displacement of [3H]5-HT from human 5HT2A receptor expressed in CHO cells | B | 7.41 | pKi | 39 | nM | Ki | Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544] |
| ChEMBL | Affinity for human 5-hydroxytryptamine 2A receptor expressed in mammalian cell line | B | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042] |
| ChEMBL | Displacement of [125I]DOI from human 5HT2A | B | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 2A receptor using displacement of [3H]5-HT | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (1997) 40: 2762-2769 [PMID:9276022] |
| ChEMBL | Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544] |
| ChEMBL | Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader | F | 6.88 | pEC50 | 131 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042] |
| ChEMBL | Binding to human 5HT2A receptor expressed in CHO cells | B | 6.88 | pEC50 | 131 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042] |
| ChEMBL | Displacement of [3H]5-HT from human 5HT2B | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207] |
| GtoPdb | - | - | 8.3 | pKi | 5.01 | nM | Ki | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| ChEMBL | Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader | F | 8.37 | pEC50 | 4.3 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042] |
| ChEMBL | Binding to human 5HT2B receptor expressed in CHO cells | B | 8.37 | pEC50 | 4.3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207] |
| ChEMBL | Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis | F | 8.62 | pEC50 | 2.4 | nM | EC50 | Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544] |
| ChEMBL | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from human 5HT2C receptor expressed in CHO cells | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544] |
| GtoPdb | - | - | 8.2 | pKi | 6.31 | nM | Ki |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Eur J Pharmacol (2004) 483: 37-43 [PMID:14709324] |
| ChEMBL | Affinity for human 5-hydroxytryptamine 2C receptor expressed in mammalian cell line | B | 8.64 | pKi | 2.3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042] |
| ChEMBL | Displacement of [3H]5-HT from human 5HT2C | B | 8.64 | pKi | 2.3 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 2C receptor using displacement of [3H]DOB | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (1997) 40: 2762-2769 [PMID:9276022] |
| ChEMBL | Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis | F | 7.28 | pEC50 | 52 | nM | EC50 | Bioorg Med Chem (2008) 16: 1966-1982 [PMID:18035544] |
| ChEMBL | Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader | F | 7.74 | pEC50 | 18 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 2367-2370 [PMID:15081042] |
| ChEMBL | Binding to human 5HT2C receptor expressed in CHO cells | B | 7.74 | pEC50 | 18 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 677-680 [PMID:16257207] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 8.4 | pEC50 | 3.98 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat | F | 6.7 | pEC50 | 199.53 | nM | EC50 | J Med Chem (1997) 40: 2762-2769 [PMID:9276022] |
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]
