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 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 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 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]
ChEMBL Inhibition of Nav1.8 (unknown origin) B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2023) 254: 115371-115371 [PMID:37084597]
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 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]