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Assay Detail

CHEMBL4844527

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Binding
Antagonist activity at 5-HT3 receptor in guinea-pig ileum assessed as inhibition of 5HT-induced contraction incubated for 15 mins
9
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL3666)
Type SINGLE PROTEIN
Organism Cavia porcellus

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
pD2 7 - -
Kd 2 7.11 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4849693 1 7.11
CHEMBL46 ONDANSETRON 4.0 2 7.11
CHEMBL4860809 1 -
CHEMBL4867565 1 -
CHEMBL4846153 1 -
CHEMBL4862354 1 -
CHEMBL4870374 1 -
CHEMBL4863272 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4849693 Kd = 77.62 nM 7.11
CHEMBL46 ONDANSETRON Kd = 77.62 nM 7.11
CHEMBL46 ONDANSETRON pD2 = 6.43 -
CHEMBL4860809 pD2 = 7.33 -
CHEMBL4867565 pD2 = 7.43 -
CHEMBL4846153 pD2 = 6.71 -
CHEMBL4862354 pD2 = 6.09 -
CHEMBL4870374 pD2 = 6.74 -
CHEMBL4863272 pD2 = 6.38 -