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Assay Detail

CHEMBL4136300

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

Binding
Agonist activity at human TLR7 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8.
Larson P, Kucaba TA, Xiong Z, Olin M, Griffith TS, Ferguson DM.
ACS Med Chem Lett (2017) 8 : 1148 -1152
PubMed 29152046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.58 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170901 1 6.75
CHEMBL4162974 1 6.22
CHEMBL383322 RESIQUIMOD 2.0 1 5.87
CHEMBL2216760 1 5.77
CHEMBL4174580 1 5.76
CHEMBL4160925 1 5.76
CHEMBL3116322 1 5.65
CHEMBL4169848 1 5.54
CHEMBL4164327 1 5.54
CHEMBL4161057 1 5.51
CHEMBL4172215 1 5.49
CHEMBL4165438 1 5.48
CHEMBL4176050 1 5.44
CHEMBL4161998 1 5.42
CHEMBL4163927 1 5.34
CHEMBL4172654 1 5.18
CHEMBL1282 IMIQUIMOD 4.0 1 4.94
CHEMBL3116325 1 4.84
CHEMBL4166427 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170901 EC50 = 180.0 nM 6.75
CHEMBL4162974 EC50 = 600.0 nM 6.22
CHEMBL383322 RESIQUIMOD EC50 = 1340.0 nM 5.87
CHEMBL2216760 EC50 = 1690.0 nM 5.77
CHEMBL4174580 EC50 = 1740.0 nM 5.76
CHEMBL4160925 EC50 = 1720.0 nM 5.76
CHEMBL3116322 EC50 = 2220.0 nM 5.65
CHEMBL4169848 EC50 = 2890.0 nM 5.54
CHEMBL4164327 EC50 = 2890.0 nM 5.54
CHEMBL4161057 EC50 = 3060.0 nM 5.51
CHEMBL4172215 EC50 = 3210.0 nM 5.49
CHEMBL4165438 EC50 = 3330.0 nM 5.48
CHEMBL4176050 EC50 = 3640.0 nM 5.44
CHEMBL4161998 EC50 = 3840.0 nM 5.42
CHEMBL4163927 EC50 = 4530.0 nM 5.34
CHEMBL4172654 EC50 = 6670.0 nM 5.18
CHEMBL1282 IMIQUIMOD EC50 = 11400.0 nM 4.94
CHEMBL3116325 EC50 = 14370.0 nM 4.84
CHEMBL4166427 EC50 = 190000.0 nM -