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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]