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Assay Detail

CHEMBL982902

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

Functional
Antagonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as inhibition of 5-hydroxytryptamine-induced increase in [35S]GTPgammaS binding
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.
Siracusa MA, Salerno L, Modica MN, Pittalà V, Romeo G, Amato ME, Nowak M, Bojarski AJ, Mereghetti I, Cagnotto A, Mennini T.
J Med Chem (2008) 51 : 4529 -4538
PubMed 18598015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.49 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476722 1 8.89
CHEMBL477200 1 8.77
CHEMBL514074 1 8.18
CHEMBL516590 1 8.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476722 Ki = 1.3 nM 8.89
CHEMBL477200 Ki = 1.7 nM 8.77
CHEMBL514074 Ki = 6.6 nM 8.18
CHEMBL516590 Ki = 7.4 nM 8.13