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: CHEMBL27846 |
---|
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 |
---|---|---|---|---|---|---|---|---|
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
ChEMBL | Binding affinity was evaluated by Alpha-1 adrenergic receptor in calf cortex by displacing prazosin | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
ChEMBL | Binding affinity was evaluated by Dopamine receptor D1 agonism in the calf striatum by displacing SCH 23390 | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
ChEMBL | Binding affinity was evaluated by Dopamine receptor D2 agonism in the calf striatum by displacing spiperone | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | The ability to inhibit [3H]domperidone binding to dopamine receptor D2 in rat striata | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity was evaluated by 5-hydroxytryptamine 1A receptor agonism in the pig cortex by displacing 8-OH-DPAT | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Binding affinity was evaluated by 5-hydroxytryptamine 2A receptor agonism in the rat cortex by displacing ketanserin | B | 5 | pKd | <5 | - | pKD | J Med Chem (1995) 38: 2326-2330 [PMID:7608898] |
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
ChEMBL | Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
ChEMBL | Binding affinity for 5-hydroxytryptamine 3 receptor by displacement of racemic [3H]zacopride from rat cortex | B | 8.43 | pKi | 3.71 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 477-480 |
ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor was determined in rat cerebro cortical membranes using [3H]quipazine. | B | 8.5 | pKi | 3.16 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1375-1378 |
ChEMBL | Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor in rat brain cortical membranes using radioligand [3H]quipazine | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (1993) 36: 2645-2657 [PMID:8410977] |
ChEMBL | Binding affinity at 5-hydroxytryptamine 3 receptor in rat posterior cortex by [3H]-BRL 43694 displacement. | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (1992) 2: 691-694 |
ChEMBL | Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement. | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1555-1558 |
ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor in rat entorhinal cortex using [3H]-BRL 43694 as radioligand | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 945-948 |
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
ChEMBL | Binding affinity for 5-hydroxytryptamine 3 receptor by displacement of [3H](R)-zacopride from ondansetron-treated NG-108-15 cell membranes | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 477-480 |
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand | B | 5.82 | pKi | 1510 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity in the rat esophageal muscularis mucosae | F | 6.3 | pEC50 | 501.19 | nM | EC50 | Bioorg Med Chem Lett (1993) 3: 1375-1378 |
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
ChEMBL | Binding affinity for 5-hydroxytryptamine 4 receptor by displacement of [3H]GR-113808 from guinea pig brain striatum. | B | 5.55 | pKi | 2818.38 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 477-480 |
ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum | F | 6.78 | pEC50 | 166 | nM | EC50 | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
5-HT3AB in Human [GtoPdb: 378] | ||||||||
GtoPdb | - | - | 7.7 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
5-HT3A in Human [GtoPdb: 379] | ||||||||
GtoPdb | - | - | 7.9 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
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]