A-381393 [Ligand Id: 8441] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL127257
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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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
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of alpha2A adrenergic receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Inhibition of alpha2C adrenergic receptor (unknown origin) B 5.72 pKi 1912 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Inhibition of human dopamine D1 receptor B 5.1 pKi >8000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Inhibition of human dopamine D2 (long) receptor (unknown origin) B 5.22 pKi >6000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Inhibition of human dopamine D3 receptor B 5.22 pKi >6000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 8.82 pKi 1.5 nM Ki Neuropharmacology (2005) 49: 112-21 [PMID:15992586]
ChEMBL In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL Inhibition of human dopamine D4 receptor B 8.82 pKi 1.5 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2004) 47: 3853-3864 [PMID:15239663]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Inhibition of human dopamine D5 receptor B 5.1 pKi >8000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Inhibition of histamine H1 receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibition of serotonin 5-HT1A receptor (unknown origin) B 5.86 pKi 1365 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Inhibition of serotonin 5-HT1B receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Inhibition of serotonin 5-HT2 receptor (unknown origin) B 6.43 pKi 370 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inhibition of serotonin 5-HT2C receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Inhibition of serotonin 5-HT6 receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Inhibition of serotonin 5-HT7 receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL Inhibition of sigma2 receptor (unknown origin) B 5.7 pKi >2000 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]