BMY-14802 [Ligand Id: 8] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL60859 (BMY-14802)
  • D2 receptor/Dopamine D2 receptor in Mouse [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Mouse [ChEMBL: CHEMBL3465] [GtoPdb: 2552] [UniProtKB: O55242]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
ChEMBL In vitro binding affinity towards dopamine receptor D2 B 5.61 pIC50 2431 nM IC50 J Med Chem (1992) 35: 4344-4361 [PMID:1360026]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity towards Dopamine receptor D2 binding site using [3H]spiroperidol. B 5.08 pIC50 8400 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
ChEMBL In vitro inhibitory against radioligand [3H]spiperone binding to rat striatal Dopamine receptor D2 B 5.19 pIC50 6430 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Binding affinity against the Dopamine receptor D2 in rat striatum by using [3H]spiperone radioligand B 5.31 pIC50 4900 nM IC50 Bioorg Med Chem Lett (1992) 2: 165-170
ChEMBL Inhibitory concentration against radioligand [3H](-)-sulpiride binding to Dopamine receptor D2 in rat B 6 pIC50 >1000 nM IC50 J Med Chem (1999) 42: 1076-1087 [PMID:10090790]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.2 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 In vitro binding affinity towards serotonin 5-HT1A receptor by the displacement of [3H]8-OH-DPAT from rat hippocampus B 6.49 pIC50 320 nM IC50 Bioorg Med Chem Lett (1994) 4: 1941-1946
ChEMBL Inhibitory concentration against radioligand [3H]8-OH-DPAT binding to rat hippocampal 5-hydroxytryptamine 1A receptor B 6.49 pIC50 320 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT. B 6.49 pIC50 320 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL In vitro binding affinity towards serotonin 5-HT2A receptor by the displacement of [3H]spiperone from rat cortical membranes B 5.77 pIC50 1700 nM IC50 Bioorg Med Chem Lett (1994) 4: 1941-1946
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin. B 6.08 pIC50 830 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer B 6.58 pKi 265 nM Ki Eur J Med Chem (2009) 44: 519-525 [PMID:18499305]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Ability to displace [3H](+)-pentazocine from Sigma opioid receptor type 1 of guinea pig brain B 6.58 pKi 265 nM Ki J Med Chem (2002) 45: 4923-4930 [PMID:12383018]
ChEMBL Binding affinity for Sigma opioid receptor type 1 in guinea pig brain homogenate with 0.5 nM [3H](+)-PENT B 6.58 pKi 265 nM Ki Bioorg Med Chem Lett (1994) 4: 2185-2188
ChEMBL Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand. B 6.58 pKi 265 nM Ki J Med Chem (2002) 45: 438-448 [PMID:11784148]
ChEMBL Binding affinity for Sigma opioid receptor type 2 in guinea pig brain homogenate with 4 nM [3H]-(+)-DTG B 6.79 pKi 164 nM Ki Bioorg Med Chem Lett (1994) 4: 2185-2188
ChEMBL Binding affinity against the sigma receptor from guinea pig brain using the radioligand [3H]SKF-10047 B 7.15 pKi 71 nM Ki Bioorg Med Chem Lett (1992) 2: 165-170
ChEMBL Inhibition of specific binding of [3H]DTG to sigma receptor in Guinea pig brain membranes B 6.92 pIC50 120 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL In vitro binding affinity towards sigma receptor by the displacement of [3H]PPP from guinea pig brain B 6.95 pIC50 112 nM IC50 Bioorg Med Chem Lett (1994) 4: 1941-1946
ChEMBL Inhibitory concentration against radioligand [3H]3-PPP binding to haloperidol-sensitive sigma binding site in whole guinea pig brain B 6.95 pIC50 112 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Inhibitory concentration against radioligand [3H](+)-NAN binding to haloperidol-sensitive sigma binding site in whole guinea pig brain B 7.08 pIC50 83 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes B 7.15 pIC50 71 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3465] [GtoPdb: 2552] [UniProtKB: O55242]
ChEMBL In vitro binding affinity for the mouse sigma opioid receptor B 6.76 pKi 174 nM Ki J Med Chem (1992) 35: 4344-4361 [PMID:1360026]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Ability to displace [3H]ditolylguanidine in the presence of 100 nM (+)-pentazocine from Sigma opioid receptor type 2 of rat liver B 6.41 pKi 391 nM Ki J Med Chem (2002) 45: 4923-4930 [PMID:12383018]
ChEMBL Sigma opioid receptor type 2 affinity in rat liver by employing [3H]ditolylguanidine as radioligand B 6.41 pKi 391 nM Ki J Med Chem (2002) 45: 438-448 [PMID:11784148]
ChEMBL Binding affinity towards Sigma receptor site 2 in rat brain using [3H]DTG as radioligand B 6.64 pIC50 230 nM IC50 J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL Inhibitory concentration against radioligand [3H]3-PPP binding to Sigma opioid receptor type 1 in rat brain membrane B 6.8 pIC50 158 nM IC50 J Med Chem (1999) 42: 1076-1087 [PMID:10090790]
ChEMBL Displacement of (+)-[3H]-3-PPP from rat cortical sigma site F 6.95 pIC50 112 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay. B 7.22 pIC50 60 nM IC50 J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine B 7.22 pIC50 60 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]

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]