Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL31354 (WAY-100635) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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] |
ChEMBL | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting | B | 7.73 | pKi | 18.62 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 7.73 | pKi | 18.62 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
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] |
ChEMBL | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1B expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter | B | 7.18 | pKi | 66.07 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 7.18 | pKi | 66.07 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
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] |
ChEMBL | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1D expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter | B | 8.34 | pKi | 4.57 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
ChEMBL | Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | B | 8.34 | pKi | 4.57 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding affinity to D4 receptor (unknown origin) assessed as dissociation constant | B | 8.62 | pKd | 2.4 | nM | Kd | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
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 | Binding affinity to 5-HT1A receptor (unknown origin) assessed as dissociation constant | B | 9.7 | pKd | 0.2 | nM | Kd | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
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 cloned 5HT-1AR transfected in HeLa cells incubated for 30 mins by liquid scintillation counter | B | 9.48 | pKi | 0.33 | nM | Ki | Eur J Med Chem (2019) 176: 310-325 [PMID:31112892] |
ChEMBL | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay | B | 9.48 | pKi | 0.33 | nM | Ki | Eur J Med Chem (2019) 168: 461-473 [PMID:30844609] |
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 | Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805] |
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 | Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat hippocampal membrane 5HT1A receptor | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
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 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]