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Assay Detail

CHEMBL2447574

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

Binding
Displacement of [3H]-prazosin from alpha1 adrenergic receptor in rat cerebral cortex membranes after 50 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.
Lacivita E, Di Pilato P, Stama ML, Colabufo NA, Berardi F, Perrone R, De Filippis B, Laviola G, Adriani W, Niso M, Leopoldo M.
Bioorg Med Chem Lett (2013) 23 : 6083 -6086
PubMed 24100077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.17 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442994 1 7.94
CHEMBL522691 1 7.65
CHEMBL2442996 1 7.52
CHEMBL2442995 1 7.42
CHEMBL2442999 1 6.71
CHEMBL2442997 1 6.53
CHEMBL2442998 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442994 Ki = 11.4 nM 7.94
CHEMBL522691 Ki = 22.6 nM 7.65
CHEMBL2442996 Ki = 30.5 nM 7.52
CHEMBL2442995 Ki = 38.3 nM 7.42
CHEMBL2442999 Ki = 193.0 nM 6.71
CHEMBL2442997 Ki = 295.0 nM 6.53
CHEMBL2442998 Ki = 393.0 nM 6.41