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Assay Detail

CHEMBL982896

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat brain cortex
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
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 7 6.83 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478413 1 7.10
CHEMBL477200 1 7.02
CHEMBL477765 1 6.97
CHEMBL517962 1 6.76
CHEMBL479026 1 6.74
CHEMBL476722 1 6.68
CHEMBL514074 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478413 Ki = 78.8 nM 7.10
CHEMBL477200 Ki = 96.1 nM 7.02
CHEMBL477765 Ki = 106.0 nM 6.97
CHEMBL517962 Ki = 174.0 nM 6.76
CHEMBL479026 Ki = 183.0 nM 6.74
CHEMBL476722 Ki = 207.0 nM 6.68
CHEMBL514074 Ki = 298.0 nM 6.53