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Assay Detail

CHEMBL5031925

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

Binding
Antagonist activity at rat P2X3 receptor
4
Total Activities
4
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

P2X purinoceptor 3 (CHEMBL4824)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Kai H, Horiguchi T, Kameyma T, Onodera N, Itoh N, Fujii Y, Ichihashi Y, Hirai K, Shintani T, Nakamura K, Minami K, Kasai E, Yoneda S, Murakami Y, Ogawa H, Sekimoto R, Shinohara S, Yoshida O, Kurose N.
Bioorg Med Chem Lett (2021) 52 : 128384 -128384
PubMed 34587541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.29 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5084053 1 8.42
CHEMBL5084939 1 8.40
CHEMBL4748113 1 8.21
CHEMBL5073093 1 8.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5084053 IC50 = 3.8 nM 8.42
CHEMBL5084939 IC50 = 4.0 nM 8.40
CHEMBL4748113 IC50 = 6.1 nM 8.21
CHEMBL5073093 IC50 = 7.7 nM 8.11