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Assay Detail

CHEMBL644686

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

Functional
Alpha-1 Adrenoceptor blocking activity as antagonism of norepinephrine-induced contractions of epididymal portion of 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-1 (CHEMBL1907610)
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 7.54 8.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351897 2 8.97
CHEMBL27013 1 8.93
CHEMBL159440 2 8.75
CHEMBL159888 1 8.61
CHEMBL162538 2 8.55
CHEMBL2 PRAZOSIN 4.0 1 8.54
CHEMBL160908 1 8.13
CHEMBL159922 2 6.07
CHEMBL606671 2 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351897 Kd = 1.072 nM 8.97
CHEMBL27013 Kd = 1.175 nM 8.93
CHEMBL159440 Kd = 1.778 nM 8.75
CHEMBL159888 Kd = 2.455 nM 8.61
CHEMBL162538 Kd = 2.818 nM 8.55
CHEMBL2 PRAZOSIN Kd = 2.884 nM 8.54
CHEMBL160908 Kd = 7.413 nM 8.13
CHEMBL351897 Kd = 26.92 nM 7.57
CHEMBL159440 Kd = 75.86 nM 7.12
CHEMBL162538 Kd = 81.28 nM 7.09
CHEMBL159922 Kd = 851.14 nM 6.07
CHEMBL606671 Kd = 1584.89 nM 5.80
CHEMBL159922 Kd = 1819.7 nM 5.74
CHEMBL606671 Kd = 2290.87 nM 5.64