(+)-WAY 100135 [Ligand Id: 126] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL38288 (WAY-100135)
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]