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Assay Detail

CHEMBL4017813

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

ADMET
Activation of PXR (unknown origin)
2
Total Activities
2
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

Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.
Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME.
Bioorg Med Chem Lett (2017) 27 : 2087 -2093
PubMed 28389149 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.03 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062780 1 5.25
CHEMBL4061793 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062780 EC50 = 5600.0 nM 5.25
CHEMBL4061793 EC50 = 16000.0 nM 4.80