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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL60859 (BMY-14802)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone from CHO-K1 cell membranes expressing human dopamine receptor D2 B 5.48 pKi 3346 nM Ki J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
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]spiperone binding to rat striatal Dopamine receptor D2 B 6 pIC50 >1000 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
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]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]-spiperone from CHO-K1 cell membranes expressing human dopamine 3 receptors B 5.7 pKi >2000 nM Ki J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
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 Inhibitory concentration against radioligand [3H]8-OH-DPAT binding to rat hippocampal 5-hydroxytryptamine 1A receptor B 6.47 pIC50 340 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
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 Tested for [3H](+)-pentazocine binding to sigma-1 receptor in guinea pig brain membrane B 6.31 pKi 490 nM Ki J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
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 Inhibitory concentration against radioligand [3H](+)-NAN binding to haloperidol-sensitive sigma binding site in whole guinea pig brain B 6.38 pIC50 420 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Inhibitory concentration against radioligand [3H]3-PPP binding to haloperidol-sensitive sigma binding site in whole guinea pig brain B 6.51 pIC50 310 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL The compound was tested for affinity towards sigma-3 receptor B 6.67 pIC50 213.8 nM IC50 J Med Chem (1994) 37: 4109-4117 [PMID:7990111]
ChEMBL Inhibitory concentration against radioligand [3H]DTG binding to haloperidol-sensitive sigma binding site in whole guinea pig brain B 6.85 pIC50 140 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
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 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 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](+)-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 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]