ChEMBL ligand: CHEMBL1242923
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] There should be some charts here, you may need to enable JavaScript!
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] There should be some charts here, you may need to enable JavaScript!
5-HT3A/5-hydroxytryptamine receptor 3A in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] There should be some charts here, you may need to enable JavaScript!
5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] There should be some charts here, you may need to enable JavaScript!
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] There should be some charts here, you may need to enable JavaScript!
A1 receptor/Adenosine receptor A1 in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] There should be some charts here, you may need to enable JavaScript!
A2A receptor/Adenosine receptor A2a in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] There should be some charts here, you may need to enable JavaScript!
A3 receptor/Adenosine receptor A3 in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] There should be some charts here, you may need to enable JavaScript!
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] There should be some charts here, you may need to enable JavaScript!
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] There should be some charts here, you may need to enable JavaScript!
α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] There should be some charts here, you may need to enable JavaScript!
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] There should be some charts here, you may need to enable JavaScript!
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase A/Amine oxidase [flavin-containing] A in Human [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] There should be some charts here, you may need to enable JavaScript!
β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] There should be some charts here, you may need to enable JavaScript!
β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] There should be some charts here, you may need to enable JavaScript!
CB1 receptor/Cannabinoid receptor 1 in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] There should be some charts here, you may need to enable JavaScript!
D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] There should be some charts here, you may need to enable JavaScript!
D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] There should be some charts here, you may need to enable JavaScript!
D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] There should be some charts here, you may need to enable JavaScript!
ETA receptor/Endothelin-1 receptor in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] There should be some charts here, you may need to enable JavaScript!
CCK2 receptor/Gastrin/cholecystokinin type B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] There should be some charts here, you may need to enable JavaScript!
Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] There should be some charts here, you may need to enable JavaScript!
CHT/High affinity choline transporter 1 in Human [ChEMBL: CHEMBL4507] [GtoPdb: 914] [UniProtKB: Q9GZV3] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] There should be some charts here, you may need to enable JavaScript!
H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] There should be some charts here, you may need to enable JavaScript!
H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] There should be some charts here, you may need to enable JavaScript!
κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] There should be some charts here, you may need to enable JavaScript!
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705] There should be some charts here, you may need to enable JavaScript!
MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245] There should be some charts here, you may need to enable JavaScript!
MT1 receptor/Melatonin receptor type 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] There should be some charts here, you may need to enable JavaScript!
M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] There should be some charts here, you may need to enable JavaScript!
M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] There should be some charts here, you may need to enable JavaScript!
M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] There should be some charts here, you may need to enable JavaScript!
M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] There should be some charts here, you may need to enable JavaScript!
M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] There should be some charts here, you may need to enable JavaScript!
μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] There should be some charts here, you may need to enable JavaScript!
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] There should be some charts here, you may need to enable JavaScript!
Y1 receptor/Neuropeptide Y receptor type 1 in Human [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929] There should be some charts here, you may need to enable JavaScript!
NTS1 receptor/Neurotensin receptor type 1 in Human [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989] There should be some charts here, you may need to enable JavaScript!
Nischarin in Human [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] There should be some charts here, you may need to enable JavaScript!
Ribosyldihydronicotinamide dehydrogenase [quinone] in Human [ChEMBL: CHEMBL3959] [UniProtKB: P16083] There should be some charts here, you may need to enable JavaScript!
DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] There should be some charts here, you may need to enable JavaScript!
NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
SERT/Sodium-dependent serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] There should be some charts here, you may need to enable JavaScript!
NK2 receptor/Substance-K receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] There should be some charts here, you may need to enable JavaScript!
NK1 receptor/Substance-P receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] There should be some charts here, you may need to enable JavaScript!
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2B 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 3A 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/5-hydroxytryptamine receptor 4 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/5-hydroxytryptamine receptor 7 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]
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 receptor A1 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 receptor A2a 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 receptor A3 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]
Monoamine oxidase A/Amine oxidase [flavin-containing] 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]
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 receptor 1 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]
D1 receptor/D(1A) dopamine 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/D(2) dopamine 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/D(3) dopamine 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/D(4) dopamine 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]
ETA receptor/Endothelin-1 receptor 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]
CCK2 receptor/Gastrin/cholecystokinin type 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]
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]
CHT/High affinity choline transporter 1 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-type 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]
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 type 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]
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 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]
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]
μ receptor/Mu-type 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]
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 type 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]
Ribosyldihydronicotinamide dehydrogenase [quinone] 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]
DAT/Sodium-dependent 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]
NET/Sodium-dependent noradrenaline 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]
SERT/Sodium-dependent 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]
NK2 receptor/Substance-K 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]
NK1 receptor/Substance-P 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]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]