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ChEMBL ligand: CHEMBL1242923 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
ChEMBL | Binding affinity to human acetylcholine esterase by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Binding affinity to human adenosine A1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Binding affinity to human adenosine A1 receptor agonist site by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Binding affinity to human adenosine A2A receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Binding affinity to human adenosine A3 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assay | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Binding affinity to human adrenergic Alpha-1B receptor by radioligand displacement assay | B | 6.04 | pKi | 910 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | Binding affinity to human adrenergic Alpha-1D receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | Binding affinity to human adrenergic alpha2A receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | Binding affinity to adrenergic alpha2B receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
ChEMBL | Binding affinity to human adrenergic beta-1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
ChEMBL | Binding affinity to adrenergic beta2 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
ChEMBL | Binding affinity to human CB1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
ChEMBL | Binding affinity to human CCK2 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Binding affinity to human dopamine D1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]raclopride from human D2L receptor expressed in CHO cells after 60 mins by scintillation proximity assay | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319] |
ChEMBL | Binding affinity to human dopamine D2S receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Binding affinity to human D2S agonist site receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Displacement of [3H]-raclopride from human dopamine D2L receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis | B | 6.08 | pKi | 834 | nM | Ki | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
ChEMBL | Displacement of [3H]-raclopride from human dopamine D2L receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis | B | 6.08 | pKi | 831.76 | nM | Ki | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Binding affinity to human dopamine D3 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding affinity to human D4.4 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | Binding affinity to human dopamine transporter by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
ChEMBL | Binding affinity to human ETA receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
ChEMBL | Binding affinity to human glucocorticoid receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319] |
CHT/High-affinity choline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4507] [GtoPdb: 914] [UniProtKB: Q9GZV3] | ||||||||
ChEMBL | Binding affinity to human choline transporter (CHT1) by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Binding affinity to human histamine H1 receptor by radioligand displacement assay | B | 6.11 | pKi | 780 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
ChEMBL | Binding affinity to human histamine H2 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Binding affinity to human histamine H3 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Binding affinity to kappa opioid receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | Binding affinity to p38alpha by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705] | ||||||||
ChEMBL | Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis | B | 5.07 | pIC50 | 8525 | nM | IC50 | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
ChEMBL | Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis | B | 5.07 | pIC50 | 8511.38 | nM | IC50 | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
ChEMBL | Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization | F | 6.89 | pEC50 | 129 | nM | EC50 | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
ChEMBL | Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization | F | 6.89 | pEC50 | 128.82 | nM | EC50 | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245] | ||||||||
ChEMBL | Binding affinity to human MC4 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
ChEMBL | Binding affinity to human MT1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
ChEMBL | Binding affinity to MAOA by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Binding affinity to human mu opioid receptor agonist site by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Binding affinity to human muscarinic M1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay | F | 7.01 | pEC50 | 97 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay | F | 7.21 | pEC50 | 61 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining | F | 7.21 | pEC50 | 61 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Binding affinity to human muscarinic M2 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Binding affinity to human muscarinic M3 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells | B | 5.16 | pKi | 6900 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Binding affinity to human muscarinic M4 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells | B | 5.05 | pKi | 8900 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Binding affinity to human muscarinic M5 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] | ||||||||
ChEMBL | Binding affinity to human NK1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
ChEMBL | Binding affinity to human NK2 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
ChEMBL | Binding affinity to nAChR alpha4beta2 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
Y1 receptor/Neuropeptide Y receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929] | ||||||||
ChEMBL | Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989] | ||||||||
ChEMBL | Binding affinity to human UT1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
ChEMBL | Binding affinity to I1 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | Binding affinity to human NE transporter by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
Quinone reductase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
ChEMBL | Binding affinity to ML2 (MT3) receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | Binding affinity to 5-HT1B receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
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 human 5-HT2A receptor expressed in F1pIn CHO cell membranes after 1 hr by scintillation counting method | B | 5.98 | pKi | 1047.13 | nM | Ki | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in F1pIn CHO cell membranes after 1 hr by scintillation counting method | B | 5.98 | pKi | 1042 | nM | Ki | J Med Chem (2015) 58: 1550-1555 [PMID:25590655] |
ChEMBL | Binding affinity to human 5-HT2A agonist site receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Binding affinity to human 5-HT2B agonist site receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Binding affinity to human 5HT2C receptor agonist site by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
ChEMBL | Binding affinity to human 5-HT3 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
ChEMBL | Binding affinity to human 5-HT4e receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Binding affinity to human 5-HT7 receptor by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Binding affinity to human 5-HT transporter by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
ChEMBL | Binding affinity to Lyn by radioligand displacement assay | B | 6 | pKi | >=1000 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
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]