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ChEMBL ligand: CHEMBL431367 (Roxindole) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | Binding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1996) 39: 3179-3187 [PMID:8759640] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
GtoPdb | - | - | 8.6 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
GtoPdb | - | - | 8.6 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
ChEMBL | Compound was evaluated for effective concentration in vivo for Dopamine receptor D2 mitogenesis. (95% confidence intervals) | F | 9.43 | pEC50 | 0.37 | nM | EC50 | J Med Chem (1996) 39: 3179-3187 [PMID:8759640] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | In vitro binding affinity for dopamine receptor D2 on rat striatal membranes by [3H]spiperone displacement. | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1997) 40: 250-259 [PMID:9003524] |
ChEMBL | Binding affinity at Dopamine receptor D2 in rat striatal membrane by [3H]spiperone displacement. | B | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (1996) 39: 3179-3187 [PMID:8759640] |
ChEMBL | Evaluated for its ability to displace tritiated receptor ligand in rat striatal membranes [3H]ADTN, a dopamine agonist | F | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (1992) 35: 4020-4026 [PMID:1359142] |
ChEMBL | Compound was evaluated for its ability to displace tritiated receptor ligand in rat striatal membranes 3[H]spiperone, a dopamine antagonist | F | 8.23 | pIC50 | 5.95 | nM | IC50 | J Med Chem (1992) 35: 4020-4026 [PMID:1359142] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor of rat striatal membranes | B | 8.25 | pIC50 | 5.6 | nM | IC50 | J Med Chem (2004) 47: 4677-4683 [PMID:15341483] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
GtoPdb | - | - | 8.9 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
ChEMBL | Binding affinity against human Dopamine receptor D3 in CHO-K1 cells using [3H]spiperone as radioligand | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (1996) 39: 3179-3187 [PMID:8759640] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (1996) 39: 3179-3187 [PMID:8759640] |
GtoPdb | - | - | 8.2 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
GtoPdb | - | - | 9.9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754]; J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
ChEMBL | Inhibition of 5HT1A receptor | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1118-1123 [PMID:20022748] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | Inhibition of 8-OH DPAT bindign to rat hydroxytryptamine 1A receptor expressed in CHO cells | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2004) 47: 4677-4683 [PMID:15341483] |
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
GtoPdb | - | - | 6 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754]; J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754]; J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
GtoPdb | - | - | 8.2 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
GtoPdb | - | - | 7.5 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
GtoPdb | - | - | 6.5 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
GtoPdb | - | - | 8.6 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
GtoPdb | - | - | 8.3 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
GtoPdb | - | - | 8.8 | pKi | - | - | - | J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666] |
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]