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Assay Detail

CHEMBL2166097

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

Binding
Displacement of [3H]prazoin from rat cerebral cortex adrenergic alpha1 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.
Lacivita E, Patarnello D, Stroth N, Caroli A, Niso M, Contino M, De Giorgio P, Di Pilato P, Colabufo NA, Berardi F, Perrone R, Svenningsson P, Hedlund PB, Leopoldo M.
J Med Chem (2012) 55 : 6375 -6380
PubMed 22738316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.12 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597 PHENTOLAMINE 4.0 1 7.80
CHEMBL494675 1 7.23
CHEMBL2164338 1 6.98
CHEMBL2164336 1 6.81
CHEMBL2164334 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597 PHENTOLAMINE Ki = 16.0 nM 7.80
CHEMBL494675 Ki = 59.1 nM 7.23
CHEMBL2164338 Ki = 105.0 nM 6.98
CHEMBL2164336 Ki = 156.0 nM 6.81
CHEMBL2164334 Ki = 165.0 nM 6.78