RU 24969 [Ligand Id: 23] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL18785 (RU-24969) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 9 | pKi | - | - | - | Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. | B | 7.96 | pKi | 10.96 | nM | Ki | J Med Chem (1993) 36: 4006-4014 [PMID:8258822] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 7.96 | pKi | 10.96 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand assay. | B | 7.96 | pKi | 10.9 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2963-2968 |
| ChEMBL | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from rat 5HT1A receptor | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2013) 63: 578-588 [PMID:23542166] |
| 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptor | B | 8.22 | pIC50 | 6 | nM | IC50 | Eur J Med Chem (2013) 63: 578-588 [PMID:23542166] |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Mol Pharmacol (1991) 40: 143-8 [PMID:1652050] |
| ChEMBL | Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1D receptor of bovine caudate using [3H]5-HT as the radioligand | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| ChEMBL | Displacement of [3H]-ketanserin from human 5HT2A receptor | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2013) 63: 578-588 [PMID:23542166] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| ChEMBL | Displacement of [3H]-mesulergine from human 5HT2C receptor | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2013) 63: 578-588 [PMID:23542166] |
| ChEMBL | Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand | B | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (1990) 33: 2087-2093 [PMID:2374139] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 6.2 | pKi | - | - | - | J Neurochem (1996) 66: 47-56 [PMID:8522988] |
| ChEMBL | Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
| 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - | FEBS Lett (1994) 355: 242-6 [PMID:7988681] |
| 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Mol Pharmacol (1993) 43: 313-9 [PMID:8450829] |
| 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
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]
