A-803467 [Ligand Id: 5734] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL250699 (A-803467)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
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  • CCK1 receptor/Cholecystokinin A receptor in Human [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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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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  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
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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-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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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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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
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  • Nav1.3/Sodium channel protein type III alpha subunit in Human [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
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  • Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Nav1.8/Sodium channel protein type X alpha subunit in Human [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
  • Nav1.8/Sodium channel protein type X alpha subunit in Mouse [ChEMBL: CHEMBL5158] [GtoPdb: 585] [UniProtKB: Q6QIY3]
  • Nav1.8/Sodium channel protein type X alpha subunit in Rat [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
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  • Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
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  • Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526]
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  • Kv7.3/Voltage-gated potassium channel subunit Kv7.3 in Human [ChEMBL: CHEMBL2684] [GtoPdb: 562] [UniProtKB: O43525]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]CGS-21680 from adenosine A2A receptor B 5 pIC50 10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [125I]AB-MECA from adenosine A3 receptor B 4.92 pIC50 12000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Displacement of [3H](-)CGP-12177 from adrenergic beta-1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Displacement of [3H]RX821002 from adrenergic alpha-2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Displacement of [3H](-)CGP-12177 from adrenergic beta2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]Win 55212-2 from cannabinoid CB1 receptor B 5 pIC50 10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]Win 55212-2 from cannabinoid CB2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
ChEMBL Displacement of [125I]MIP1-alpha from CCR1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
CCK1 receptor/Cholecystokinin A receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238]
ChEMBL Binding affinity to CCKAR B 5.7 pIC50 >2000 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]DADLE from opioid delta receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Displacement of [3H]SCH-23390 from dopamine D1 receptor B 5.15 pIC50 7000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Binding affinity to dopamine D1 receptor B 5.7 pIC50 >2000 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]spiperone from dopamine D3 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]spiperone from dopamine D4.4 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Displacement of [3H]SCH23390 from dopamine D5 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
ChEMBL Displacement of [125I]endothelin-1 from endothelin ETA receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]pyrilamine from histamine H1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Displacement of [125I]APT from histamine H2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
ChEMBL Displacement of [125I]IL8 from CXCR2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U-69593 from opioid kappa receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from opioid mu receptor B 5 pIC50 10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Displacement of [3H]pirezepine from muscarinic M1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Displacement of [3H]AF-DX384 from muscarinic M2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Displacement of [3H]4DAMP from muscarinic M3 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Displacement of [3H]4DAMP from muscarinic M4 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Displacement of [3H]4DAMP from muscarinic M5 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Displacement of [3H]nociceptin from ORL1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
P2X2/P2X purinoceptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2531] [GtoPdb: 479] [UniProtKB: Q9UBL9]
ChEMBL Displacement of [3H]alpha,beta-methyl ATP from P2X receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of P2X2 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373]
ChEMBL Inhibition of P2X3 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
ChEMBL Displacement of [35S]dATP-alpha-S from P2Y receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]8OH-DPAT from 5HT1A receptor B 5 pIC50 10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Displacement of [3H]CYP from 5HT1B receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor B 5.52 pIC50 3000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Binding affinity to 5HT2A receptor B 5.7 pIC50 >2000 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]mesulergine from 5HT2C receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Displacement of [3H]BRL43694 from 5HT3 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Displacement of [3H]LSD from 5HT5A receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]LSD from 5HT6 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]LSD from 5HT7 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Displacement of [3H]pentazocine from sigma1 receptor B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
ChEMBL Inhibition of human Nav1.2 channel expressed in HEK293 cells at -120 mV by patch clamp method B 5.02 pIC50 9490 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of human recombinant NaV1.2 by electrophysiology B 5.13 pIC50 7400 nM IC50 Bioorg Med Chem (2010) 18: 7816-7825 [PMID:20965738]
ChEMBL Inhibition of human Nav1.2 channel expressed in HEK293 cells at -60 mV by patch clamp method B 5.13 pIC50 7380 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of inactivated human Nav1.2 sodium channel B 5.14 pIC50 7180 nM IC50 J Med Chem (2007) 50: 2583-2588 [PMID:17489575]
Nav1.3/Sodium channel protein type III alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
ChEMBL Inhibition of human Nav1.3 channel expressed in HEK293 cells at -120 mV by patch clamp method B 4.93 pIC50 11760 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of inactivated human Nav1.3 sodium channel B 5.61 pIC50 2450 nM IC50 J Med Chem (2007) 50: 2583-2588 [PMID:17489575]
ChEMBL Inhibition of human Nav1.3 channel expressed in HEK293 cells at -60 mV by patch clamp method B 5.61 pIC50 2450 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Inhibition of human Nav1.7 channel expressed in HEK293 cells at -120 mV by patch clamp method B 4.45 pIC50 35340 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of inactivated human Nav1.7 sodium channel B 5.17 pIC50 6740 nM IC50 J Med Chem (2007) 50: 2583-2588 [PMID:17489575]
ChEMBL Inhibition of human Nav1.7 channel expressed in HEK293 cells at -60 mV by patch clamp method B 5.17 pIC50 6740 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of human Nav1.5 channel expressed in HEK293 cells at -150 mV by patch clamp method B 4.48 pIC50 32820 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of inactivated human Nav1.5 sodium channel B 5.13 pIC50 7440 nM IC50 J Med Chem (2007) 50: 2583-2588 [PMID:17489575]
ChEMBL Inhibition of human Nav1.5 channel expressed in HEK293 cells at -90 mV by patch clamp method B 5.13 pIC50 7340 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of human Nav1.5 channel at 1 uM B 5.7 pIC50 >2000 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
Nav1.8/Sodium channel protein type X alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
ChEMBL Inhibition of human Nav1.8 channel expressed in HEK293 cells at -100 mV by patch clamp method B 7.1 pIC50 79 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of human recombinant Nav 1.8 channel expressed in HEK293 cells B 8.1 pIC50 8 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
ChEMBL Inhibition of inactivated human Nav1.8 sodium channel B 8.1 pIC50 8 nM IC50 J Med Chem (2007) 50: 2583-2588 [PMID:17489575]
ChEMBL Inhibition of human Nav1.8 channel expressed in human HEK293 cells by patch clamp method B 8.1 pIC50 8 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of human Nav1.8 channel expressed in HEK293 cells at -40 mV by patch clamp method B 8.1 pIC50 8 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assay B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2010) 18: 7816-7825 [PMID:20965738]
Nav1.8/Sodium channel protein type X alpha subunit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5158] [GtoPdb: 585] [UniProtKB: Q6QIY3]
ChEMBL Inhibition of mouse recombinant Nav 1.8 channel expressed in HEK293 cells by isotopic efflux assay B 6.07 pIC50 850 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
ChEMBL Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay B 6.07 pIC50 850 nM IC50 Bioorg Med Chem (2010) 18: 7816-7825 [PMID:20965738]
Nav1.8/Sodium channel protein type X alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
ChEMBL Inhibition of Nav1.8 channel in rat dorsal root ganglion neurons assessed as blockade of TTX-R current at -100 mV by patch clamp method B 6 pIC50 1000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of Nav1.8 channel in rat dorsal root ganglion neurons assessed as blockade of TTX-R current by patch clamp method B 6.85 pIC50 140 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
ChEMBL Inhibition of tetrodotoxin-resistant NaV1.8 in rat dorsal root ganglion neurons at holding potential -100 mV by whole-cell patch clamp electrophysiology assay B 6.85 pIC50 140 nM IC50 Bioorg Med Chem (2010) 18: 7816-7825 [PMID:20965738]
ChEMBL Inhibition of tetrodotoxin-resistant NaV1.8 in rat DRG neuron by electrophysiology B 6.9 pIC50 125 nM IC50 Bioorg Med Chem Lett (2010) 20: 6812-6815 [PMID:20855211]
ChEMBL Inhibition of recombinant rat Nav1.8 sodium channel assessed as blockade of TTXR current by patch clamp method B 7.35 pIC50 45 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
GtoPdb - - 8.1 pIC50 8 nM IC50 Proc Natl Acad Sci USA (2007) 104: 8520-5 [PMID:17483457]
Translocator protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5742] [GtoPdb: 2879] [UniProtKB: P30536]
ChEMBL Binding affinity to peripheral benzodiazepine receptor B 5.7 pIC50 >2000 nM IC50 J Med Chem (2008) 51: 407-416 [PMID:18176998]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Inhibition of TRPV1 B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
ChEMBL Inhibition of Cav2.2 channel B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526]
ChEMBL Inhibition of KCNQ2 channel B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Kv7.3/Voltage-gated potassium channel subunit Kv7.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2684] [GtoPdb: 562] [UniProtKB: O43525]
ChEMBL Inhibition of KCNQ3 channel B 5 pIC50 >10000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]