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 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]
