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Assay Detail

CHEMBL4035080

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

Binding
Antagonist activity at human TLR7 expressed in HEK293 cells assessed as inhibition of CL264-induced NF-kappaB activation after 24 hrs by spectrophotometry based SEAP reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Toll-like receptor 7 (CHEMBL5936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and development of benzoxazole derivatives with toll-like receptor 9 antagonism.
Roy S, Mukherjee A, Paul B, Rahaman O, Roy S, Maithri G, Ramya B, Pal S, Ganguly D, Talukdar A.
Eur J Med Chem (2017) 134 : 334 -347
PubMed 28437629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.12 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065452 1 5.70
CHEMBL4082132 1 5.34
CHEMBL4100657 1 5.33
CHEMBL4067391 1 5.30
CHEMBL4088644 1 5.12
CHEMBL4100138 1 5.09
CHEMBL4073879 1 5.08
CHEMBL4071152 1 4.96
CHEMBL4084216 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065452 IC50 = 1990.0 nM 5.70
CHEMBL4082132 IC50 = 4570.0 nM 5.34
CHEMBL4100657 IC50 = 4710.0 nM 5.33
CHEMBL4067391 IC50 = 4990.0 nM 5.30
CHEMBL4088644 IC50 = 7550.0 nM 5.12
CHEMBL4100138 IC50 = 8090.0 nM 5.09
CHEMBL4073879 IC50 = 8300.0 nM 5.08
CHEMBL4071152 IC50 = 10840.0 nM 4.96
CHEMBL4084216 IC50 = 66170.0 nM 4.18