ChEMBL ligand: CHEMBL1621 (9-hydroxyrisperidone, Invega, NSC-759623, Paliperidona, Paliperidone, R-76477, Risperidone impurity, 9-hydroxyrisperidone-, RO-76477, RO76477)
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-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] 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-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-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!
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!
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!
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] There should be some charts here, you may need to enable JavaScript!
Kv4.3/A-type voltage-gated potassium channel KCND3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17] 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!
D5 receptor/D(1B) dopamine receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] 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!
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!
Nav1.5/Sodium channel protein type 5 subunit alpha in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] 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	Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL	Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant	B	6.95	pKi	111	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL	Binding affinity to 5HT1D receptor (unknown origin) assessed as inhibition constant	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Binding affinity to 5HT2A (unknown origin) assessed as inhibition constant	B	9.08	pKi	0.83	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL	Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	F	8.28	pIC50	5.2	nM	IC50	Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Binding affinity to 5HT2C receptor (unknown origin) assessed as inhibition constant	B	7.72	pKi	19	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Binding affinity to 5HT7 receptor (unknown origin) assessed as inhibition constant	B	8.17	pKi	6.8	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Binding affinity to alpha1A adrenergic receptor (unknown origin) assessed as inhibition constant	B	7.96	pKi	11	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL	Binding affinity to alpha2A adrenergic receptor (unknown origin) assessed as inhibition constant	B	7.96	pKi	11	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL	Binding affinity to alpha2B adrenergic receptor (unknown origin) assessed as inhibition constant	B	8.4	pKi	4	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL	Binding affinity to alpha2C adrenergic receptor (unknown origin) assessed as inhibition constant	B	8.57	pKi	2.7	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
Kv4.3/A-type voltage-gated potassium channel KCND3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
ChEMBL	Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform	F	4.2	pIC50	63095.73	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Binding affinity to D1 receptor (unknown origin) assessed as inhibition constant	B	6.26	pKi	554	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
D5 receptor/D(1B) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL	Binding affinity to D5 receptor (unknown origin) assessed as inhibition constant	B	7.54	pKi	29	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Binding affinity to D2 receptor (unknown origin) assessed as inhibition constant	B	8.8	pKi	1.6	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL	Antagonist activity at dopamine D2 receptor (unknown origin) after 60 mins by Ultra lance cAMP assay	F	8.08	pIC50	8.28	nM	IC50	Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Binding affinity to D3 receptor (unknown origin) assessed as inhibition constant	B	8.12	pKi	7.5	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Binding affinity to D4 receptor (unknown origin) assessed as inhibition constant	B	7.42	pKi	38	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL	Binding affinity to H1 receptor (unknown origin) assessed as inhibition constant	B	7.47	pKi	34	nM	Ki	J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
Nav1.5/Sodium channel protein type 5 subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL	Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform	F	4.6	pIC50	25118.86	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
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 channel	B	5.89	pIC50	1300	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	Inhibition of human ERG channel	B	5.89	pIC50	1300	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	Inhibition of human ERG	B	5.89	pIC50	1288.25	nM	IC50	Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL	Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform	F	5.9	pIC50	1258.93	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL	Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay	F	5.9	pIC50	1258.93	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL	Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform	F	6	pIC50	1000	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

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]