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Assay Detail

CHEMBL643746

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

Binding
Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.
Bolognesi ML, Budriesi R, Cavalli A, Chiarini A, Gotti R, Leonardi A, Minarini A, Poggesi E, Recanatini M, Rosini M, Tumiatti V, Melchiorre C.
J Med Chem (1999) 42 : 4214 -4224
PubMed 10514291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.13 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25554 1 9.37
CHEMBL135973 1 7.44
CHEMBL134428 1 7.11
CHEMBL13647 BMY-7378 1 6.42
CHEMBL135974 1 6.41
CHEMBL132378 1 6.02
CHEMBL56 8-OH-DPAT 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25554 Ki = 0.4266 nM 9.37
CHEMBL135973 Ki = 36.31 nM 7.44
CHEMBL134428 Ki = 77.62 nM 7.11
CHEMBL13647 BMY-7378 Ki = 380.19 nM 6.42
CHEMBL135974 Ki = 389.05 nM 6.41
CHEMBL132378 Ki = 954.99 nM 6.02
CHEMBL56 8-OH-DPAT Ki < 1000.0 nM -