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Assay Detail

CHEMBL876575

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Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor was determined by the displacement of [3H]prazosin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors.
Mewshaw RE, Meagher KL, Zhou P, Zhou D, Shi X, Scerni R, Smith D, Schechter LE, Andree TH.
Bioorg Med Chem Lett (2002) 12 : 307 -310
PubMed 11814784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.29 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421027 1 9.72
CHEMBL104229 1 9.05
CHEMBL322915 1 8.55
CHEMBL318604 1 8.44
CHEMBL105204 1 8.39
CHEMBL104144 1 8.33
CHEMBL105390 1 7.52
CHEMBL318738 1 7.48
CHEMBL442391 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421027 Ki = 0.19 nM 9.72
CHEMBL104229 Ki = 0.9 nM 9.05
CHEMBL322915 Ki = 2.8 nM 8.55
CHEMBL318604 Ki = 3.6 nM 8.44
CHEMBL105204 Ki = 4.1 nM 8.39
CHEMBL104144 Ki = 4.7 nM 8.33
CHEMBL105390 Ki = 30.0 nM 7.52
CHEMBL318738 Ki = 33.0 nM 7.48
CHEMBL442391 Ki = 78.0 nM 7.11