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Assay Detail

CHEMBL643687

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

Functional
Antagonist activity for Alpha-2 adrenergic receptor against clonidine in rat vas deferences
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
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. Effect of replacing a piperazine ring with an alkanediamine moiety on alpha 1-adrenoreceptor blocking activity.
Giardinà D, Brasili L, Gregori M, Massi M, Picchio MT, Quaglia W, Melchiorre C.
J Med Chem (1989) 32 : 50 -55
PubMed 2562855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 5.96 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27013 1 6.84
CHEMBL348491 1 6.68
CHEMBL150193 1 6.55
CHEMBL359103 1 6.50
CHEMBL150726 1 6.45
CHEMBL149399 1 6.31
CHEMBL153056 1 5.95
CHEMBL155341 1 5.76
CHEMBL154980 1 5.73
CHEMBL153576 1 5.52
CHEMBL2 PRAZOSIN 4.0 1 5.43
CHEMBL355968 1 5.04
CHEMBL153390 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27013 Kd = 144.54 nM 6.84
CHEMBL348491 Kd = 208.93 nM 6.68
CHEMBL150193 Kd = 281.84 nM 6.55
CHEMBL359103 Kd = 316.23 nM 6.50
CHEMBL150726 Kd = 354.81 nM 6.45
CHEMBL149399 Kd = 489.78 nM 6.31
CHEMBL153056 Kd = 1122.02 nM 5.95
CHEMBL155341 Kd = 1737.8 nM 5.76
CHEMBL154980 Kd = 1862.09 nM 5.73
CHEMBL153576 Kd = 3019.95 nM 5.52
CHEMBL2 PRAZOSIN Kd = 3715.35 nM 5.43
CHEMBL355968 Kd = 9120.11 nM 5.04
CHEMBL153390 Kd = 16595.87 nM 4.78