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Assay Detail

CHEMBL4424686

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

ADMET
Inhibition of CYP2C9 (unknown origin)
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Tobinaga H, Kameyama T, Asahi K, Horiguchi T, Oohara M, Tada Y, Fuchino K, Jikihara S, Endoh T, Kurihara N, Kanda Y, Ogawa M, Tamura N, Yagi S, Taniguchi E, Takahara Y, Shimada S, Takeyama C, Yamamoto S, Shinohara S, Kai H.
Bioorg Med Chem Lett (2019) 29 : 688 -693
PubMed 30728111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.96 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4459785 1 5.40
CHEMBL4592312 1 5.30
CHEMBL4466252 1 5.10
CHEMBL4465467 1 5.10
CHEMBL4457637 1 5.10
CHEMBL4537290 1 5.05
CHEMBL4565775 1 4.89
CHEMBL4562022 1 4.82
CHEMBL4526549 1 4.77
CHEMBL4459391 1 4.75
CHEMBL4459015 1 4.75
CHEMBL4454941 1 4.75
CHEMBL4439812 1 4.72
CHEMBL4572081 1 -
CHEMBL4445659 1 -
CHEMBL4456152 1 -
CHEMBL4437131 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4459785 IC50 = 4000.0 nM 5.40
CHEMBL4592312 IC50 = 5000.0 nM 5.30
CHEMBL4466252 IC50 = 8000.0 nM 5.10
CHEMBL4465467 IC50 = 8000.0 nM 5.10
CHEMBL4457637 IC50 = 8000.0 nM 5.10
CHEMBL4537290 IC50 = 9000.0 nM 5.05
CHEMBL4565775 IC50 = 13000.0 nM 4.89
CHEMBL4562022 IC50 = 15000.0 nM 4.82
CHEMBL4526549 IC50 = 17000.0 nM 4.77
CHEMBL4459391 IC50 = 18000.0 nM 4.75
CHEMBL4459015 IC50 = 18000.0 nM 4.75
CHEMBL4454941 IC50 = 18000.0 nM 4.75
CHEMBL4439812 IC50 = 19000.0 nM 4.72
CHEMBL4572081 IC50 > 20000.0 nM -
CHEMBL4445659 IC50 > 20000.0 nM -
CHEMBL4456152 IC50 > 20000.0 nM -
CHEMBL4437131 IC50 > 20000.0 nM -