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Assay Detail

CHEMBL4844534

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT<sub>3</sub> and 5-HT<sub>6</sub> Receptor Antagonist with Antipsychotic and Procognitive Properties.
Zajdel P, Grychowska K, Mogilski S, Kurczab R, Satała G, Bugno R, Kos T, Gołębiowska J, Malikowska-Racia N, Nikiforuk A, Chaumont-Dubel S, Bantreil X, Pawłowski M, Martinez J, Subra G, Lamaty F, Marin P, Bojarski AJ, Popik P.
J Med Chem (2021) 64 : 13279 -13298
PubMed 34467765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.20 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4867565 1 6.36
CHEMBL4870374 1 6.12
CHEMBL4846153 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4867565 Ki = 437.0 nM 6.36
CHEMBL4870374 Ki = 760.0 nM 6.12
CHEMBL4846153 Ki = 773.0 nM 6.11