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Assay Detail

CHEMBL2340586

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

Binding
Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting
3
Total Activities
3
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

Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
Gomes TF, Pompeu TE, Rodrigues DA, Noël F, Menegatti R, Andrade CH, Sabino JR, Gil ES, Dalla Costa T, Betti AH, Antonio CB, Rates SM, Fraga CA, Barreiro EJ, de Oliveira V.
Eur J Med Chem (2013) 62 : 214 -221
PubMed 23353740 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.98 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.70
CHEMBL597601 1 5.17
CHEMBL2333732 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 20.0 nM 7.70
CHEMBL597601 Ki = 6820.0 nM 5.17
CHEMBL2333732 Ki = 8220.0 nM 5.08