ChEMBL ligand: CHEMBL423294 (Cyclazosin)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130] α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] 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] α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] 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] α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] There should be some charts here, you may need to enable JavaScript!
Beta casein in Rat [ChEMBL: CHEMBL2210] [UniProtKB: P02665] There should be some charts here, you may need to enable JavaScript!
D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] 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!

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 was tested on human Alpha-1A adrenergic receptor	B	7.6	pKi	25.12	nM	Ki	J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL	Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells	B	7.91	pKi	12.3	nM	Ki	Bioorg Med Chem (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL	Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method	B	7.91	pKi	12.3	nM	Ki	Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL	Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb	-	-	8.9	pKi	-	-	-	J Med Chem (1996) 39: 4602-7 [PMID:8917649]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL	Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay	B	8.62	pKi	2.4	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL	Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat	F	7.48	pKd	33.11	nM	Kd	Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL	Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction	F	7.77	pKd	16.98	nM	Kd	Bioorg Med Chem (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL	Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride	F	7.77	pKd	16.98	nM	Kd	Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL	Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference	F	8.91	pKd	1.23	nM	Kd	J Med Chem (2009) 52: 4951-4954 [PMID:19719240]
ChEMBL	Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay	B	8.77	pKi	1.7	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	Binding affinity to human alpha1B adrenergic receptor	B	9.16	pKi	0.69	nM	Ki	Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL	Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells	B	9.49	pKi	0.32	nM	Ki	J Med Chem (2009) 52: 4951-4954 [PMID:19719240]
ChEMBL	Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay	B	9.51	pKi	0.31	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL	Binding affinity was tested on cloned hamster Alpha-1B adrenergic receptor	B	9.7	pKi	0.2	nM	Ki	J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL	Displacement of [3H]prazosin from human adrenergic alpha-1b receptor expressed in CHO cells	B	9.87	pKi	0.13	nM	Ki	Bioorg Med Chem (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL	Displacement of [3H]prazosin from human alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method	B	9.87	pKi	0.13	nM	Ki	Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
GtoPdb	-	-	9.9	pKi	-	-	-	J Med Chem (1996) 39: 4602-7 [PMID:8917649]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL	Antagonistic affinity against Alpha-1B adrenergic receptor was determined in isolated spleen tissue from rat	F	9.16	pKd	0.69	nM	Kd	Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL	Antagonist activity at rat Alpha-1B adrenoceptor assessed as inhibition if phenylephrine-induced contraction of spleen	F	9.18	pKd	0.66	nM	Kd	J Med Chem (2009) 52: 4951-4954 [PMID:19719240]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL	Binding affinity was tested on cloned rat Alpha-1D adrenergic receptor	B	7.5	pKi	31.62	nM	Ki	J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL	Displacement of [3H]prazosin from human adrenergic alpha-1d receptor expressed in CHO cells	B	8.49	pKi	3.24	nM	Ki	Bioorg Med Chem (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL	Displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method	B	8.49	pKi	3.24	nM	Ki	Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL	Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells	B	9.77	pKi	0.17	nM	Ki	J Med Chem (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb	-	-	9.9	pKi	-	-	-	J Med Chem (1996) 39: 4602-7 [PMID:8917649]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL	Antagonist activity against adrenergic Alpha-1D receptor in rat thoracic aorta assessed as noradrenaline-induced response	F	7.27	pKd	53.7	nM	Kd	Bioorg Med Chem (2007) 15: 2334-2345 [PMID:17276073]
ChEMBL	Antagonist activity at alpha1D adrenergic receptor in Wistar rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction measured after 30 mins in presence of cocaine hydrochloride and beta-adrenoceptor blocker propranolol hydrochloride	F	7.27	pKd	53.7	nM	Kd	Bioorg Med Chem (2018) 26: 3502-3513 [PMID:29784274]
ChEMBL	Antagonistic affinity against Alpha-1D adrenergic receptor was determined in isolated thoracic aorta from rat	F	7.57	pKd	26.92	nM	Kd	Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765]
ChEMBL	Antagonist activity at rat Alpha-1D adrenoceptor assessed as inhibition if norepenephrine-induced contraction of thoracic aorta	F	9.21	pKd	0.62	nM	Kd	J Med Chem (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb	-	-	7.6	pKi	-	-	-	J Med Chem (1996) 39: 4602-7 [PMID:8917649]
ChEMBL	Compound was tested for binding affinity against cloned Alpha-1D adrenergic receptor from rat brain.	B	9.24	pKi	0.58	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]
Beta casein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2210] [UniProtKB: P02665]
ChEMBL	Compound was tested for binding affinity against native Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay	B	9.85	pKi	0.14	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL	Compound was tested for binding affinity against native Dopamine receptor D2 from rat striatum using radioligand [3H]-spiperone)	B	5	pKi	<10000	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]
ChEMBL	Antagonistic affinity against rat striatum Dopamine receptor D2	F	5.08	pKi	8317.64	nM	Ki	Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Antagonistic affinity against cloned human 5-hydroxytryptamine 1A receptor	F	6	pKi	<1000	nM	Ki	Bioorg Med Chem Lett (1998) 8: 1353-1358 [PMID:9871765]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Binding affinity against native 5-HT1A-receptors from rat hippocampus using radioligand ([3H]8-hydroxy-2-(di-n-propylamino)-tetraline) binding assay	B	5.21	pKi	6165.95	nM	Ki	J Med Chem (1996) 39: 4602-4607 [PMID:8917649]

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]