(+)-WAY 100135 [Ligand Id: 126] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38288 (WAY-100135) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro binding affinity towards Dopamine receptor D2 in rat striatum was determined using [3H]-spiperone as radioligand | B | 6.41 | pKi | 389.05 | nM | Ki | J Med Chem (1995) 38: 4044-4055 [PMID:7562940] |
| ChEMBL | In vitro radioligand binding assay on Dopamine receptor D2 of rat striatum using [3H]- spiperone | B | 6.75 | pKi | 176 | nM | Ki | J Med Chem (1997) 40: 1252-1257 [PMID:9111299] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 8.9 | pKd | 1.26 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay | F | 7.77 | pIC50 | 16.9 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity at 5-hydroxytryptamine 1A receptor | B | 7.49 | pKi | 32.36 | nM | Ki | J Med Chem (1995) 38: 4044-4055 [PMID:7562940] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor | B | 7.55 | pKi | 27.9 | nM | Ki | J Med Chem (1997) 40: 1252-1257 [PMID:9111299] |
| ChEMBL | In vitro radioligand binding assay on 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT in rat hippocampus | B | 7.47 | pIC50 | 33.9 | nM | IC50 | J Med Chem (1997) 40: 1252-1257 [PMID:9111299] |
| ChEMBL | In vitro binding affinity towards the 5-hydroxytryptamine 1A receptor was evaluated | B | 7.81 | pIC50 | 15.5 | nM | IC50 | J Med Chem (1993) 36: 1509-1510 [PMID:8496920] |
| ChEMBL | In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1994) 37: 4572-4575 [PMID:7799409] |
| 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Br J Pharmacol (1997) 121: 737-42 [PMID:9208142] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity at 5-hydroxytryptamine 1B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1995) 38: 4044-4055 [PMID:7562940] |
| 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 7.6 | pKi | - | - | - | Br J Pharmacol (1997) 121: 737-42 [PMID:9208142] |
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]
