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Assay Detail

CHEMBL5135992

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

Binding
Antagonist activity at ODN2006 stimulated human TRL9 overexpressed in HEK293 cells assessed as inhibition of NF kappa B/Ap-1 activation preincubated with compound for 30 mins followed by ODN2006 stimulation measured after 22 hrs by SEAP reporter assay
10
Total Activities
10
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 9 (CHEMBL5804)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).
Sreekantha RK, Mussari CP, Dodd DS, Pasunoori L, Hegde S, Posy SL, Critton D, Ruepp S, Subramanian M, Salter-Cid LM, Tagore DM, Sarodaya S, Dudhgaonkar S, Poss MA, Schieven GL, Carter PH, Macor JE, Dyckman AJ.
ACS Med Chem Lett (2022) 13 : 812 -818
PubMed 35586440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.01 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201891 1 6.46
CHEMBL4647818 1 6.37
CHEMBL4645620 1 6.30
CHEMBL5189004 1 6.24
CHEMBL5192984 1 6.20
CHEMBL5209157 1 6.09
CHEMBL5173429 1 5.82
CHEMBL4636988 1 5.72
CHEMBL5189738 1 5.55
CHEMBL5197502 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201891 IC50 = 350.0 nM 6.46
CHEMBL4647818 IC50 = 430.0 nM 6.37
CHEMBL4645620 IC50 = 500.0 nM 6.30
CHEMBL5189004 IC50 = 570.0 nM 6.24
CHEMBL5192984 IC50 = 630.0 nM 6.20
CHEMBL5209157 IC50 = 820.0 nM 6.09
CHEMBL5173429 IC50 = 1500.0 nM 5.82
CHEMBL4636988 IC50 = 1900.0 nM 5.72
CHEMBL5189738 IC50 = 2800.0 nM 5.55
CHEMBL5197502 IC50 = 4600.0 nM 5.34