ChEMBL ligand: CHEMBL4592045 (Btrx-335140, BTRX-335140, CYM-53093, Navacaprant)
δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] There should be some charts here, you may need to enable JavaScript!
μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] 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
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL	Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay	B	5.19	pIC50	6500	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
GtoPdb	-	-	5.19	pIC50	6500	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay	B	9	pIC50	1	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL	Displacement of [3H]diprenorphine from human KOR	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
ChEMBL	Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay	B	9.1	pIC50	0.8	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
GtoPdb	-	-	9.1	pIC50	0.8	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
ChEMBL	Agonist activity at KOR (unknown origin)	F	6.39	pEC50	410	nM	EC50	Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Binding affinity to human MOR	B	6.35	pKi	450	nM	Ki	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
ChEMBL	Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay	B	6.96	pIC50	110	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
GtoPdb	-	-	6.96	pIC50	110	nM	IC50	J Med Chem (2019) 62: 1761-1780 [PMID:30707578]
ChEMBL	Agonist activity at MOR (unknown origin)	B	5.34	pEC50	4590	nM	EC50	Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400]

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]