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: CHEMBL15928 (GR-127935) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | Affinity towards cloned Opioid receptor delta 1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Binding affinity against dopamine receptor D1 | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Affinity towards cloned Dopamine receptor D1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Binding affinity against dopamine D2 receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Affinity towards cloned Dopamine receptor D2 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Binding affinity against dopamine D3 receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Affinity towards cloned Dopamine receptor D3 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding affinity against dopamine D4 receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Affinity towards cloned Dopamine receptor D4 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Affinity towards cloned Dopamine receptor D5 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Affinity towards cloned Histamine H1 receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Affinity towards cloned Opioid receptor kappa 1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Affinity towards cloned Opioid receptor mu 1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Affinity towards cloned Muscarinic acetylcholine receptor M1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity against muscarinic M1 receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Affinity towards cloned Muscarinic acetylcholine receptor M2 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity against muscarinic M2 receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Affinity towards cloned Muscarinic acetylcholine receptor M3 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity against muscarinic M3 receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
ChEMBL | Affinity towards cloned Muscarinic acetylcholine receptor M4 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Affinity towards cloned Muscarinic acetylcholine receptor M5 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT1A receptor using [3H]5-carboximidotryptamine as radioligand | B | 7.1 | pKi | 80 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Affinity for 5-hydroxytryptamine 1A receptor subtype | B | 7.14 | pKi | 72 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3183-3188 |
ChEMBL | Affinity towards cloned human 5-hydroxytryptamine 1A receptor | B | 7.15 | pKi | 70 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
GtoPdb | - | - | 7.2 | pKi | - | - | - |
J Med Chem (1997) 40: 3974-8 [PMID:9397179]; Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567] |
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 in rat hippocampus with [3H]8-OH-DPAT | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Inhibition activity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using radio binding assays | B | 6.37 | pIC50 | 425 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand. | B | 6.44 | pIC50 | 360 | nM | IC50 | J Med Chem (2000) 43: 1149-1157 [PMID:10737747] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand | B | 8.37 | pKi | 4.31 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 1B receptor | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
GtoPdb | - | - | 9.2 | pKi | - | - | - | Eur J Pharmacol (1999) 380: 171-81 [PMID:10513577] |
GtoPdb | - | - | 9.8 | pKi | - | - | - |
J Med Chem (1997) 40: 3974-8 [PMID:9397179]; Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567]; Br J Pharmacol (1998) 125: 202-8 [PMID:9776361]; Eur J Pharmacol (1996) 314: 365-72 [PMID:8957260]; J Med Chem (1998) 41: 1218-35 [PMID:9548813] |
ChEMBL | Affinity for 5-hydroxytryptamine 1B receptor subtype | B | 9.85 | pKi | 0.14 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3183-3188 |
ChEMBL | Affinity towards cloned human 5-hydroxytryptamine 1B receptor | B | 9.85 | pKi | 0.14 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand. | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2000) 43: 1149-1157 [PMID:10737747] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT1D receptor using [3H]5-carboximidotryptamine as radioligand | B | 7.91 | pKi | 12.3 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 1D receptor | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
GtoPdb | - | - | 8.6 | pKi | - | - | - | Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor alpha | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
GtoPdb | - | - | 9.1 | pKi | - | - | - |
J Med Chem (1997) 40: 3974-8 [PMID:9397179]; Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567]; Br J Pharmacol (1998) 125: 202-8 [PMID:9776361]; Eur J Pharmacol (1996) 314: 365-72 [PMID:8957260]; J Med Chem (1998) 41: 1218-35 [PMID:9548813] |
ChEMBL | Affinity for 5-hydroxytryptamine 1D receptor subtype | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3183-3188 |
ChEMBL | Affinity towards cloned human 5-hydroxytryptamine 1D receptor | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor beta | B | 9.9 | pKi | 0.13 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
ChEMBL | Inhibition affinity against 5-HT-1D receptor in bovine caudate nucleus using radio binding assay | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4297] [GtoPdb: 3] [UniProtKB: Q61224] | ||||||||
ChEMBL | Tested for 5-hydroxytryptamine receptor uptake | F | 5 | pKi | <10000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine 1D receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand. | B | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2000) 43: 1149-1157 [PMID:10737747] |
Serotonin 1d (5-HT1d) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304407] [UniProtKB: Q60484] | ||||||||
ChEMBL | In vitro binding affinity towards 5-hydroxytryptamine 1D receptor in guinea-pig striatum in presence of BMY-7378 and mesulergine | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT2A receptor using [3H]5-carboximidotryptamine as radioligand | B | 7.37 | pKi | 42.7 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 2A receptor | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
GtoPdb | - | - | 7.8 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567]; J Med Chem (1998) 41: 1218-35 [PMID:9548813] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT2C receptor using [3H]5-carboximidotryptamine as radioligand | B | 6.98 | pKi | 105 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
GtoPdb | - | - | 7 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567] |
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
ChEMBL | Binding affinity against the 5-hydroxytryptamine 3 receptor | B | 5.2 | pKi | 6309.57 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
ChEMBL | Binding affinity against 5-hydroxytryptamine 4 receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1994) 37: 2253-2257 [PMID:8057272] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
GtoPdb | - | - | 5.8 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | In vitro binding affinity towards cloned human 5-HT7 receptor using [3H]5-carboximidotryptamine as radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Inhibition of 5-hydroxytryptamine reuptake | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
GtoPdb | - | - | 5.4 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567] |
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567]; Naunyn Schmiedebergs Arch Pharmacol (2005) 371: 169-77 [PMID:15900510] |
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
GtoPdb | - | - | 6.2 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1997) 356: 312-20 [PMID:9303567] |
ChEMBL data shown on this page come from version 32:
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]