RU 24969 [Ligand Id: 23] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL18785 (RU-24969)
  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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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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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
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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 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]