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Assay Detail

CHEMBL5370441

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

Binding
Agonist activity at TLR7 in human Ramos-blue cells assessed as increase in NFkappaB activation incubated for 72 hrs by quanti-blue/SEAP reporter gene based assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and Optimization of 1-Substituted Imidazo[4,5-<i>c</i>]quinoline TLR7 Agonists.
DeYoung EG, Howe JM, Fang S, Reddy MM, Handel JP, Gillen Miller JT, Wheeler DR, Tumey LN.
ACS Med Chem Lett (2023) 14 : 1358 -1368
PubMed 37849530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.64 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5439905 1 7.75
CHEMBL5405415 1 7.41
CHEMBL5424404 1 7.36
CHEMBL5396405 1 7.23
CHEMBL5419915 1 7.21
CHEMBL5423654 1 7.16
CHEMBL5424893 1 7.08
CHEMBL5433548 1 6.97
CHEMBL5436292 1 6.78
CHEMBL5408883 1 6.75
CHEMBL5393892 1 6.70
CHEMBL5434429 1 6.68
CHEMBL5414036 1 6.64
CHEMBL5400489 1 6.63
CHEMBL5406767 1 6.56
CHEMBL5434936 1 6.46
CHEMBL5396643 1 6.31
CHEMBL5439729 1 6.27
CHEMBL383322 RESIQUIMOD 2.0 1 6.21
CHEMBL5433089 1 6.08
CHEMBL5436371 1 5.88
CHEMBL5399142 1 5.87
CHEMBL5414341 1 5.75
CHEMBL5408203 1 5.69
CHEMBL5418029 1 -
CHEMBL5436701 1 -
CHEMBL5409098 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5439905 EC50 = 18.0 nM 7.75
CHEMBL5405415 EC50 = 39.0 nM 7.41
CHEMBL5424404 EC50 = 44.0 nM 7.36
CHEMBL5396405 EC50 = 59.0 nM 7.23
CHEMBL5419915 EC50 = 62.0 nM 7.21
CHEMBL5423654 EC50 = 69.0 nM 7.16
CHEMBL5424893 EC50 = 84.0 nM 7.08
CHEMBL5433548 EC50 = 107.0 nM 6.97
CHEMBL5436292 EC50 = 168.0 nM 6.78
CHEMBL5408883 EC50 = 176.0 nM 6.75
CHEMBL5393892 EC50 = 199.0 nM 6.70
CHEMBL5434429 EC50 = 209.0 nM 6.68
CHEMBL5414036 EC50 = 231.0 nM 6.64
CHEMBL5400489 EC50 = 232.0 nM 6.63
CHEMBL5406767 EC50 = 275.0 nM 6.56
CHEMBL5434936 EC50 = 344.0 nM 6.46
CHEMBL5396643 EC50 = 485.0 nM 6.31
CHEMBL5439729 EC50 = 540.0 nM 6.27
CHEMBL383322 RESIQUIMOD EC50 = 616.0 nM 6.21
CHEMBL5433089 EC50 = 840.0 nM 6.08
CHEMBL5436371 EC50 = 1310.0 nM 5.88
CHEMBL5399142 EC50 = 1340.0 nM 5.87
CHEMBL5414341 EC50 = 1800.0 nM 5.75
CHEMBL5408203 EC50 = 2060.0 nM 5.69
CHEMBL5418029 EC50 > 30000.0 nM -
CHEMBL5436701 EC50 > 30000.0 nM -
CHEMBL5409098 EC50 > 30000.0 nM -