ChEMBL ligand: CHEMBL266195 (Alprenolol, NSC-759561)
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] Beta-2 adrenergic receptor in Bovine [ChEMBL: CHEMBL3373] [UniProtKB: Q28044] There should be some charts here, you may need to enable JavaScript!
β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] There should be some charts here, you may need to enable JavaScript!
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] There should be some charts here, you may need to enable JavaScript!
squalene synthase /Squalene synthetase in Rat [ChEMBL: CHEMBL3815] [GtoPdb: 645] [UniProtKB: Q02769] 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
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL	Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	6.75	pKd	177.83	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells	B	7.95	pKd	11.22	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	8.37	pKd	4.27	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.	B	8.31	pIC50	4.88	nM	IC50	J Med Chem (1982) 25: 931-936 [PMID:6126588]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL	Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis	B	8.84	pKd	1.45	nM	Kd	J Med Chem (2019) 62: 7806-7839 [PMID:31298548]
ChEMBL	Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis	B	8.84	pKd	1.45	nM	Kd	J Med Chem (2019) 62: 7806-7839 [PMID:31298548]
ChEMBL	Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis	B	9.1	pKd	0.79	nM	Kd	ACS Med Chem Lett (2013) 4: 1005-1010 [PMID:24454993]
ChEMBL	Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells	B	9.3	pKd	0.5	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	9.53	pKd	0.3	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis	B	8.92	pKi	1.2	nM	Ki	J Med Chem (2019) 62: 7806-7839 [PMID:31298548]
ChEMBL	Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis	B	8.92	pKi	1.2	nM	Ki	J Med Chem (2019) 62: 7806-7839 [PMID:31298548]
GtoPdb	-	-	9	pKi	-	-	-	Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]
ChEMBL	Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis	B	9	pKi	1	nM	Ki	ACS Med Chem Lett (2013) 4: 1005-1010 [PMID:24454993]
ChEMBL	Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method	B	9.3	pKi	0.5	nM	Ki	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay	F	8.26	pIC50	5.5	nM	IC50	J Med Chem (2019) 62: 7806-7839 [PMID:31298548]
ChEMBL	Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF	B	8.48	pIC50	3.3	nM	IC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins	F	8.94	pIC50	1.15	nM	IC50	J Med Chem (2019) 62: 7806-7839 [PMID:31298548]
Beta-2 adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3373] [UniProtKB: Q28044]
ChEMBL	Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.	B	8.53	pIC50	2.98	nM	IC50	J Med Chem (1982) 25: 931-936 [PMID:6126588]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL	Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells	B	6.86	pKd	138.04	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	7.12	pKd	75.86	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Displacement of [3H]-OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method	B	7.67	pKi	21.6	nM	Ki	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL	Antagonist activity at human 5HT1A expressed in BAF3 cells by fluorimetry analysis	B	6.2	pIC50	630	nM	IC50	Medchemcomm (2019) 10: 974-984 [PMID:31303996]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement	B	6.93	pKi	117.49	nM	Ki	J Med Chem (1996) 39: 126-134 [PMID:8568799]
squalene synthase /Squalene synthetase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3815] [GtoPdb: 645] [UniProtKB: Q02769]
ChEMBL	Inhibition of rat microsomal squalene synthase	B	5.38	pIC50	4200	nM	IC50	J Med Chem (1995) 38: 4157-4160 [PMID:7473541]

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]