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Assay Detail

CHEMBL643949

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

Functional
Alpha-2 Adrenoceptor blocking activity as antagonism of clonidine-induced depression of field-stimulated prostatic rat vas deferens
14
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Vas deferens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure-activity relationships in prazosin-related compounds. 2. Role of the piperazine ring on alpha-blocking activity.
Giardinà D, Gulini U, Massi M, Piloni MG, Pompei P, Rafaiani G, Melchiorre C.
J Med Chem (1993) 36 : 690 -698
PubMed 8096245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 14 5.56 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27013 1 6.84
CHEMBL159440 2 6.41
CHEMBL159922 2 5.96
CHEMBL160908 1 5.94
CHEMBL162538 2 5.91
CHEMBL606671 2 5.54
CHEMBL2 PRAZOSIN 4.0 1 5.43
CHEMBL159888 1 5.28
CHEMBL351897 2 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27013 Kd = 144.54 nM 6.84
CHEMBL159440 Kd = 389.05 nM 6.41
CHEMBL159922 Kd = 1096.48 nM 5.96
CHEMBL160908 Kd = 1148.15 nM 5.94
CHEMBL162538 Kd = 1230.27 nM 5.91
CHEMBL606671 Kd = 2884.03 nM 5.54
CHEMBL2 PRAZOSIN Kd = 3715.35 nM 5.43
CHEMBL606671 Kd = 3890.45 nM 5.41
CHEMBL159888 Kd = 5248.07 nM 5.28
CHEMBL351897 Kd = 7079.46 nM 5.15
CHEMBL351897 Kd = 8317.64 nM 5.08
CHEMBL162538 Kd = 8912.51 nM 5.05
CHEMBL159922 Kd = 9120.11 nM 5.04
CHEMBL159440 Kd = 13803.84 nM 4.86