A-381393 [Ligand Id: 8441] 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: CHEMBL127257 |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Inhibition of alpha2A adrenergic receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Inhibition of alpha2C adrenergic receptor (unknown origin) | B | 5.72 | pKi | 1912 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Inhibition of human dopamine D1 receptor | B | 5.1 | pKi | >8000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Inhibition of human dopamine D2 (long) receptor (unknown origin) | B | 5.22 | pKi | >6000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | Displacement of [3H]-spiperone from human D2 receptor assessed as inhibition constant | B | 5.22 | pKi | >6000 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Inhibition of human dopamine D3 receptor | B | 5.22 | pKi | >6000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | Displacement of [3H]-spiperone from human D3 receptor assessed as inhibition constant | B | 5.22 | pKi | >6000 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| GtoPdb | - | - | 8.82 | pKi | 1.5 | nM | Ki | Neuropharmacology (2005) 49: 112-21 [PMID:15992586] |
| ChEMBL | In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Inhibition of human dopamine D4 receptor | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant | B | 8.82 | pKi | 1.5 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| ChEMBL | In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Inhibition of human dopamine D5 receptor | B | 5.1 | pKi | >8000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Inhibition of histamine H1 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT1A receptor (unknown origin) | B | 5.86 | pKi | 1365 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT1B receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT2 receptor (unknown origin) | B | 6.43 | pKi | 370 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT2C receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT6 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT7 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | Inhibition of sigma2 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
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]
