(+)-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 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]
