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ChEMBL ligand: CHEMBL60859 (BMY-14802) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]