ChEMBL ligand: CHEMBL596 (AD 923, AD-923, Breakyl, Duragesic, Duragesic-100, Duragesic-12, Duragesic-25, Duragesic-37, Duragesic-50, Duragesic-75, Durogesic, Durogesic d-trans, Durogesic dtrans, En3267, EN-3267, Fencino, Fendrop, Fentalis reservoir, Fentanest, Fentanilo, Fentanyl, Fentanyl-100, Fentanyl-12, Fentanyl-25, Fentanyl-37, Fentanyl-50, Fentanyl-62, Fentanyl-75, Fentanyl-87, Fentanyl cii, Fentanyl component of tranq, IDS-NF-001, Innovar, Matrifen, Mezolar matrix, Mylafent, N02AB03, Opiodur, Oralet, Osmach, Osmanil, Phentanyl, R 4263, Recivit, Recuvyra, Sublimase, Subsys, Tilofyl, Victanyl, Yemex)
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!
ABCB1/ATP-dependent translocase ABCB1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] 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!
δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] δ receptor/Delta-type opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] δ receptor/Delta-type opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] 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] Kappa-type opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144] 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] μ receptor/Mu-type opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] μ receptor/Mu-type opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] Mu-type opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266] There should be some charts here, you may need to enable JavaScript!
NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] Sigma non-opioid intracellular receptor 1 in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] There should be some charts here, you may need to enable JavaScript!
Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] 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
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Binding affinity to recombinant human alpha-1A-Adr expressed in HEK cells assessed as inhibition constant	B	5.85	pKi	1407	nM	Ki	J Med Chem (2024) 67: 603-619 [PMID:38156970]
ChEMBL	Antagonist activity at recombinant human alpha-1A-Adr expressed in HEK cells assessed as inhibition constant preincubated for 10 mins followed by tamsulosin addition measured after 1 hr by ELISA	F	5.44	pIC50	3660	nM	IC50	J Med Chem (2024) 67: 603-619 [PMID:38156970]
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	Binding affinity to recombinant human alpha-1B-Adr expressed in HEK cells assessed as inhibition constant	B	5.96	pKi	1100	nM	Ki	J Med Chem (2024) 67: 603-619 [PMID:38156970]
ChEMBL	Antagonist activity at recombinant human alpha-1B-Adr expressed in HEK cells assessed as inhibition constant preincubated for 10 mins followed by tamsulosin addition measured after 1 hr by ELISA	F	5.43	pIC50	3690	nM	IC50	J Med Chem (2024) 67: 603-619 [PMID:38156970]
ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	F	5.19	pIC50	6500	nM	IC50	Anesthesiology (2002) 96: 913-920 [PMID:11964599]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	4.68	pKi	21000	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	4.58	pKi	26200	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	6.26	pKi	554	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL	Binding affinity against Opioid receptor delta 1	B	5.99	pKi	1035	nM	Ki	J Med Chem (2000) 43: 381-391 [PMID:10669565]
ChEMBL	Binding affinity against Opioid receptor delta 1 in guinea pig brain membranes	B	6.17	pKi	679	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
ChEMBL	Displacement of [3H]DPDPE from human delta opioid receptor	B	6.24	pKi	570	nM	Ki	Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
GtoPdb	-	-	6.8	pKi	-	-	-	NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL	Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand	B	6.37	pIC50	431	nM	IC50	J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL	In vitro binding activity against opioid receptor delta using [3DPDPE] as radioligand	B	6.73	pIC50	187.4	nM	IC50	J Med Chem (1991) 34: 827-841 [PMID:1847432]
ChEMBL	Compound was tested in vitro for binding affinity towards delta opioid receptor by measuring displacement of [3H]DPDPE from guinea pig brain membranes	B	6.73	pIC50	187	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1177-1182
ChEMBL	Agonist activity at human DOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis	F	6.82	pIC50	150.03	nM	IC50	J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
δ receptor/Delta-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL	Displacement of [3H]-DPDPE from Swiss Webster mouse neural membranes delta opioid receptor after 60 mins by liquid scintillation spectrometric analysis	B	6.25	pKi	568	nM	Ki	Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
ChEMBL	Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electric stimulation-induced contraction	B	5.03	pIC50	9400	nM	IC50	Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
ChEMBL	Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated muscle contraction	B	8.02	pIC50	9.5	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL	Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction	F	8.02	pIC50	9.45	nM	IC50	J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL	Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction	B	8.03	pIC50	9.4	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL	Agonist activity at delta opioid receptor in beta-funaltrexamine-treated mouse vas deferens	B	8.46	pIC50	3.45	nM	IC50	Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
δ receptor/Delta-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL	Binding affinity towards Opioid receptor delta 1 using [3H]DADLE as radioligand.	B	5.99	pKi	1035	nM	Ki	J Med Chem (1995) 38: 1547-1557 [PMID:7739013]
ChEMBL	Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane	B	6.25	pKi	568	nM	Ki	J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL	Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain	B	6.4	pKi	400	nM	Ki	J Med Chem (2003) 46: 623-633 [PMID:12570383]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting	B	4.7	pIC50	19952.62	nM	IC50	J Med Chem (2012) 55: 7054-7060 [PMID:22793499]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL	Binding affinity against Opioid receptor kappa 1	B	6.71	pKi	196.5	nM	Ki	J Med Chem (2000) 43: 381-391 [PMID:10669565]
GtoPdb	-	-	7.1	pKi	-	-	-	NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL	Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand	B	5.8	pIC50	1580	nM	IC50	J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL	Agonist activity at human KOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis	F	6.01	pEC50	987.35	nM	EC50	J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
Kappa-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL	Binding affinity against Opioid receptor kappa 1 in guinea pig brain membranes	B	5.95	pKi	1130	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
ChEMBL	Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane	B	6.53	pKi	298	nM	Ki	J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL	Binding affinity towards Opioid receptor kappa 1 using [3H]U-69593 as radioligand.	B	6.71	pKi	196.5	nM	Ki	J Med Chem (1995) 38: 1547-1557 [PMID:7739013]
ChEMBL	In vitro binding activity against opioid receptor kappa using [3H]EKC as radioligand	B	5.23	pIC50	5893	nM	IC50	J Med Chem (1991) 34: 827-841 [PMID:1847432]
ChEMBL	Compound was tested in vitro for binding affinity towards kappa opioid receptor by measuring displacement of [3H]EKC from guinea pig brain membranes	B	5.23	pIC50	5893	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1177-1182
μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay	B	8.28	pKi	5.23	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL	Binding affinity against Opioid receptor mu 1	B	8.4	pKi	3.97	nM	Ki	J Med Chem (2000) 43: 381-391 [PMID:10669565]
ChEMBL	Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 90 mins measured by MicroBeta scintillation counter method	B	8.48	pKi	3.3	nM	Ki	Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067]
ChEMBL	Displacement of [3H]DAMGO (2 nM ) from opioid receptor mu 1 in human brain	B	8.54	pKi	2.9	nM	Ki	Bioorg Med Chem Lett (2004) 14: 491-493 [PMID:14698188]
ChEMBL	Displacement of [3H]DAMGO from human mu opioid receptor measured after 2 hrs by competitive binding assay	B	8.87	pKi	1.35	nM	Ki	J Med Chem (2022) 65: 13483-13504 [PMID:36206553]
ChEMBL	Binding affinity to mu opioid receptor (unknown origin) expressed in HEK cells at pH 7.4	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2018) 61: 5822-5880 [PMID:29400967]
GtoPdb	-	-	9.2	pKi	-	-	-	NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL	Binding affinity to MOR (unknown origin) assessed as inhibition constant	B	10.08	pKi	0.08	nM	Ki	J Med Chem (2024) 67: 603-619 [PMID:38156970]
ChEMBL	Binding affinity to mu-opioid receptor (unknown origin) assessed as inhibition constant	B	10.29	pKi	0.05	nM	Ki	J Med Chem (2023) 66: 6463-6497 [PMID:37145921]
ChEMBL	Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay	F	7.97	pIC50	10.72	nM	IC50	ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209]
ChEMBL	Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay	F	8.26	pIC50	5.5	nM	IC50	ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209]
ChEMBL	Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand	B	8.89	pIC50	1.3	nM	IC50	J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL	Agonist activity at human MOR expressed in CHO-K1 cells assessed as decrease in beta-arrestin 2 recruitment incubated for 90 mins by HitHunter cAMP analysis	F	7.24	pEC50	57.2	nM	EC50	J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
ChEMBL	Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay	B	7.28	pEC50	53	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL	Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay	F	7.37	pEC50	43	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL	Displacement of [35S]GTP-gammaS from MOR (unknown origin)	B	7.65	pEC50	22.6	nM	EC50	J Med Chem (2024) 67: 603-619 [PMID:38156970]
ChEMBL	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	F	7.76	pEC50	17.38	nM	EC50	J Med Chem (2020) 63: 15709-15725 [PMID:33271020]
ChEMBL	Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay	F	7.76	pEC50	17.2	nM	EC50	J Med Chem (2020) 63: 15709-15725 [PMID:33271020]
ChEMBL	Agonist activity at human mu opioid receptor expressed in CHO cells co-transfected with human Galpha16 assessed as intracellular calcium concentration incubated for 24 hrs by FLIPR calcium 4 assay	F	8.32	pEC50	4.79	nM	EC50	J Med Chem (2024) 67: 10447-10463 [PMID:38869493]
ChEMBL	Agonist activity at mu-opioid receptor (unknown origin)	F	8.72	pEC50	1.9	nM	EC50	J Med Chem (2023) 66: 16257-16275 [PMID:38015878]
ChEMBL	Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay	F	8.72	pEC50	1.9	nM	EC50	J Med Chem (2023) 66: 16257-16275 [PMID:38015878]
ChEMBL	Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay	F	9.29	pEC50	0.51	nM	EC50	ACS Med Chem Lett (2019) 10: 1568-1572 [PMID:31749912]
ChEMBL	Agonist activity at human MOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis	F	9.68	pEC50	0.21	nM	EC50	J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
μ receptor/Mu-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL	Displacement of [3H]-DAMGO from Swiss Webster mouse neural membranes mu opioid receptor after 60 mins by liquid scintillation spectrometric analysis	B	8.23	pKi	5.9	nM	Ki	Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
ChEMBL	Agonist activity at mouse MOR expressed in CHO cells incubated for 15 mins by calcium mobilization assay	F	6.88	pEC50	133	nM	EC50	J Med Chem (2024) 67: 603-619 [PMID:38156970]
μ receptor/Mu-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL	Displacement of [3H] DAMGO from rat mu-opioid receptor	B	6.24	pKi	570	nM	Ki	Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane	B	8.23	pKi	5.9	nM	Ki	J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL	Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes	B	8.23	pKi	5.9	nM	Ki	Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
ChEMBL	Binding affinity towards Opioid receptor mu 1 using [3H]DAMGO as radioligand.	B	8.4	pKi	3.97	nM	Ki	J Med Chem (1995) 38: 1547-1557 [PMID:7739013]
ChEMBL	Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane.	B	8.67	pKi	2.16	nM	Ki	J Med Chem (1989) 32: 663-671 [PMID:2563773]
ChEMBL	Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes.	B	8.67	pKi	2.16	nM	Ki	J Med Chem (1990) 33: 2876-2882 [PMID:2170652]
ChEMBL	Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2003) 46: 623-633 [PMID:12570383]
GtoPdb	-	-	9.4	pKi	-	-	-	Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]
ChEMBL	Displacement of [3H] DAMGO from rat mu-opioid receptor	B	5.9	pIC50	1258.93	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL	Displacement of [3H]DAMGO from rat brain mu opioid receptor incubated for 60 mins by microbeta scintillation counting method	B	8.91	pIC50	1.23	nM	IC50	Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
ChEMBL	Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor	F	7.49	pEC50	32.4	nM	EC50	Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
Mu-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL	Binding affinity against mu opioid receptor in guinea pig brain membranes	B	8.07	pKi	8.45	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
ChEMBL	Agonist activity at mu opioid receptor in guinea pig isolated ileum assessed as inhibition of electric stimulation-induced contraction	B	5.47	pIC50	3400	nM	IC50	Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
ChEMBL	Agonist activity at mu opioid receptor in beta-funaltrexamine-treated guinea pig isolated ileum	B	8.02	pIC50	9.45	nM	IC50	Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
ChEMBL	Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction	F	8.46	pIC50	3.45	nM	IC50	J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL	Inhibition of mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction	B	8.47	pIC50	3.4	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL	Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically stimulated muscle contraction	B	8.47	pIC50	3.4	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL	Compound was tested in vitro for binding affinity towards mu opioid receptor by measuring displacement of [3H]DAGO from guinea pig brain membranes	B	8.51	pIC50	3.1	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1177-1182
ChEMBL	In vitro binding activity against opioid receptor mu using [3H]-DAGO as radioligand	B	8.51	pIC50	3.1	nM	IC50	J Med Chem (1991) 34: 827-841 [PMID:1847432]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL	Agonist activity at human NOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis	F	5	pEC50	>10000	nM	EC50	J Med Chem (2024) 67: 9173-9193 [PMID:38810170]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Inhibition of sigma 1 receptor (unknown origin)	B	9.41	pKi	0.39	nM	Ki	Eur J Med Chem (2020) 191: 112144-112144 [PMID:32087465]
ChEMBL	Displacement of [3H]PPP from sigma1 receptor (unknown origin)	B	6.45	pIC50	354	nM	IC50	Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL	Displacement of [3H]SKF10047 from rat brain sigma1 receptor incubated for 35 mins by scintillation counting method	B	6	pKi	>1000	nM	Ki	Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
Sigma non-opioid intracellular receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes by microbeta scintillation counting method	B	5.61	pKi	2474.3	nM	Ki	Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067]
ChEMBL	Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method	B	5.3	pIC50	4973	nM	IC50	Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL	Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis	B	4.34	pIC50	46170	nM	IC50	J Med Chem (2019) 62: 9890-9905 [PMID:31597043]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibitory concentration against potassium channel HERG	B	5.74	pIC50	1819.7	nM	IC50	Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]

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]