WAY-100635 [Ligand Id: 80] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL31354 (WAY-100635)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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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/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Mouse [ChEMBL: CHEMBL4297] [GtoPdb: 3] [UniProtKB: Q61224]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Inhibition of adrenergic alpha1A receptor B 7.7 pKi 20 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique B 7.73 pKi 18.62 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Inhibition of adrenergic Alpha-1B receptor B 6.49 pKi 322 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique B 7.18 pKi 66.07 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Displacement [3H]prazosin of human recombinant Alpha-1D adrenergic receptor expressed in CHO cells by rapid filtration technique B 8.34 pKi 4.57 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Inhibition of dopamine D4 receptor B 7.8 pKi 16 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
GtoPdb - - 7.8 pKi 16 nM Ki J. Med. Chem. (2011) 54: 3480-91 [PMID:21520940]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibition of 5HT1A receptor B 8.66 pKi 2.2 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins B 8.66 pKi 2.2 nM Ki J. Med. Chem. (2009) 52: 7892-7896 [PMID:19705871]
ChEMBL Binding affinity against human 5-hydroxytryptamine 1A receptor in CHO cells labeled with [3H]8-OH-DPAT radioligand B 9.02 pKi 0.96 nM Ki J. Med. Chem. (2004) 47: 3823-3842 [PMID:15239661]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2010) 53: 4066-4084 [PMID:20443629]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells B 9.05 pKi 0.9 nM Ki Bioorg. Med. Chem. (2008) 16: 6707-6723 [PMID:18571421]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2009) 52: 4955-4959 [PMID:19719241]
ChEMBL Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor B 9.1 pKi 0.79 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
GtoPdb - - 9.2 pKi 0.63 nM Ki Eur. J. Pharmacol. (1998) 355: 245-56 [PMID:9760039];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 205-17 [PMID:9550290]
ChEMBL In vitro inhibition of [3H]- 8-OH-DPAT binding to cloned cell line containing human 5-hydroxytryptamine 1A receptor B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1999) 42: 1576-1586 [PMID:10229627]
ChEMBL Binding affinity at human 5-hydroxytryptamine 1A receptor by inhibition of [3H]8-OH-DPAT binding in Chinese hamster ovary cell line B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2002) 45: 165-176 [PMID:11754589]
ChEMBL Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting B 9.41 pKi 0.39 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique B 9.48 pKi 0.33 nM Ki Eur. J. Med. Chem. (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor B 9.8 pKi 0.16 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay F 7.95 pIC50 11.3 nM IC50 J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level F 8.15 pIC50 7.1 nM IC50 J. Med. Chem. (2010) 53: 4066-4084 [PMID:20443629]
ChEMBL Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting B 9.04 pIC50 0.91 nM IC50 J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor F 8.15 pEC50 7.1 nM EC50 J. Med. Chem. (2004) 47: 3823-3842 [PMID:15239661]
ChEMBL Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells B 8.15 pEC50 7.1 nM EC50 J. Med. Chem. (2004) 47: 3823-3842 [PMID:15239661]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes. F 9.69 pKd 0.2 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 2457-2462 [PMID:9873561]
ChEMBL In vitro binding affinity for 5-hydroxytryptamine 1A receptor was determined by measuring specific inhibition of [125I]-binding to rat hippocampal membrane preparations B 10 pKd 0.1 nM Kd J. Med. Chem. (1998) 41: 157-166 [PMID:9457239]
ChEMBL Inhibition of binding of [125I]8-OH-PIPAT ligand to 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates B 9.08 pKi 0.84 nM Ki J. Med. Chem. (1994) 37: 1406-1407 [PMID:8182697]
ChEMBL Compound was tested for inhibition constant against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes. B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2457-2462 [PMID:9873561]
ChEMBL In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate B 8.66 pIC50 2.2 nM IC50 J. Med. Chem. (1994) 37: 4572-4575 [PMID:7799409]
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates B 8.66 pIC50 2.2 nM IC50 J. Med. Chem. (1994) 37: 1406-1407 [PMID:8182697]
ChEMBL In vitro affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT in rat hippocampus B 9.43 pIC50 0.37 nM IC50 J. Med. Chem. (2000) 43: 432-439 [PMID:10669570]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Inhibition of 5HT1B receptor B 7.62 pKi 24 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4297] [GtoPdb: 3] [UniProtKB: Q61224]
ChEMBL Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 1) F 8.96 pKi 1.09 nM Ki J. Med. Chem. (1999) 42: 1576-1586 [PMID:10229627]
ChEMBL Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 2) F 9.47 pKi 0.34 nM Ki J. Med. Chem. (1999) 42: 1576-1586 [PMID:10229627]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Inhibition of 5HT7 receptor B 5 pKi 10000 nM Ki J. Med. Chem. (2011) 54: 3480-3491 [PMID:21520940]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells B 5.35 pIC50 >4500 nM IC50 J. Med. Chem. (2004) 47: 3823-3842 [PMID:15239661]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Binding affinity against serotonin transporter in rat cortical tissues using radioligand [3H]paroxetine B 6 pKi >1000 nM Ki J. Med. Chem. (2004) 47: 3823-3842 [PMID:15239661]

ChEMBL data shown on this page come from version 27:

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]