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: CHEMBL222301 |
---|
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 |
---|---|---|---|---|---|---|---|---|
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | Displacement of [3H]SCH-23390 from rat striatum dopamine D1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Displacement of [3H]spiperone from rat striatum dopamine D2 receptor | B | 5.89 | pKi | 1285 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
ChEMBL | Displacement of [3H]7OH-DPAT from rat olfactory tubercle dopamine D3 receptor | B | 5.31 | pKi | 4900 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
ChEMBL | Displacement of [3H]WIN-35428 from rat striatum DAT | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
ChEMBL | Displacement of [3H]CGP-39653 from rat cortex NMDA receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
ChEMBL | Displacement of [3H]pyrilamine from rat cortex histamine H1 receptor | B | 5.85 | pKi | 1422 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Displacement of [3H]ketanserin from rat cortex 5HT2A receptor | B | 5.5 | pKi | 3149 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Displacement of [3H]mesulergine from guinea pig cortex 5HT2C receptor | B | 5.36 | pKi | 4357 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563] | ||||||||
ChEMBL | Displacement of [3H]LY278584 from rat cortex 5HT3 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
ChEMBL | Displacement of [3H]GR-13808 from guinea pig cortex 5HT4 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
ChEMBL | Displacement of [3H]5HT from rat cloned 5HT6 receptor expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
ChEMBL | Displacement of [3H]citalopram from rat cortex SERT | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
ChEMBL | Displacement of [3H](+)-pentazocine from guinea pig sigma1 opioid receptor by liquid scintillation counting | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2010) 53: 5881-5885 [PMID:20684615] |
ChEMBL | Displacement of [3H](+)-pentazocine from guinea pig brain sigma 1 receptor | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2007) 50: 951-961 [PMID:17328523] |
sigma non-opioid intracellular receptor 1 in Human [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
GtoPdb | - | - | 8.8 | pKi | - | - | - | J Med Chem (2007) 50: 951-61 [PMID:17328523] |
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]