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Assay Detail

CHEMBL641536

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonistic activity against Alpha-2 adrenergic receptor in the prostatic portion of the rat vas deferens
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
Caroon JM, Clark RD, Kluge AF, Olah R, Repke DB, Unger SH, Michel AD, Whiting RL.
J Med Chem (1982) 25 : 666 -670
PubMed 6124635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 20 6.63 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597 PHENTOLAMINE 4.0 1 8.03
CHEMBL10347 RAUWOLSCINE 1 7.92
CHEMBL543467 IDAZOXAN HYDROCHLORIDE 1 7.80
CHEMBL15245 YOHIMBINE 3.0 1 7.71
CHEMBL31836 PIPEROXAN 2.0 1 7.40
CHEMBL1204368 1 7.00
CHEMBL1203734 1 6.84
CHEMBL1203727 1 6.84
CHEMBL578481 IMILOXAN HYDROCHLORIDE -1.0 1 6.71
CHEMBL1203725 1 6.70
CHEMBL1203738 1 6.58
CHEMBL1203739 1 6.57
CHEMBL1203715 1 6.21
CHEMBL1203742 1 6.20
CHEMBL1237158 1 6.10
CHEMBL434858 1 6.00
CHEMBL1237152 1 5.60
CHEMBL1203729 1 5.51
CHEMBL162087 1 5.50
CHEMBL1203743 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597 PHENTOLAMINE Kd = 9.333 nM 8.03
CHEMBL10347 RAUWOLSCINE Kd = 12.02 nM 7.92
CHEMBL543467 IDAZOXAN HYDROCHLORIDE Kd = 15.85 nM 7.80
CHEMBL15245 YOHIMBINE Kd = 19.5 nM 7.71
CHEMBL31836 PIPEROXAN Kd = 39.81 nM 7.40
CHEMBL1204368 Kd = 100.0 nM 7.00
CHEMBL1203734 Kd = 144.54 nM 6.84
CHEMBL1203727 Kd = 144.54 nM 6.84
CHEMBL578481 IMILOXAN HYDROCHLORIDE Kd = 194.98 nM 6.71
CHEMBL1203725 Kd = 199.53 nM 6.70
CHEMBL1203738 Kd = 263.03 nM 6.58
CHEMBL1203739 Kd = 269.15 nM 6.57
CHEMBL1203715 Kd = 616.6 nM 6.21
CHEMBL1203742 Kd = 630.96 nM 6.20
CHEMBL1237158 Kd = 794.33 nM 6.10
CHEMBL434858 Kd = 1000.0 nM 6.00
CHEMBL1237152 Kd = 2511.89 nM 5.60
CHEMBL1203729 Kd = 3090.3 nM 5.51
CHEMBL162087 Kd = 3162.28 nM 5.50
CHEMBL1203743 Kd = 3981.07 nM 5.40