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ChEMBL ligand: CHEMBL250699 (A-803467) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]