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Assay Detail

CHEMBL4136302

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Binding
Agonist activity at human TLR8 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay
9
Total Activities
9
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 8 (CHEMBL5805)
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 9 4.95 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162974 1 5.66
CHEMBL4162585 1 5.42
CHEMBL4170901 1 5.27
CHEMBL383322 RESIQUIMOD 2.0 1 5.21
CHEMBL3116322 1 5.00
CHEMBL2216760 1 4.68
CHEMBL4173277 1 4.57
CHEMBL3116325 1 4.43
CHEMBL4159198 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162974 EC50 = 2210.0 nM 5.66
CHEMBL4162585 EC50 = 3850.0 nM 5.42
CHEMBL4170901 EC50 = 5340.0 nM 5.27
CHEMBL383322 RESIQUIMOD EC50 = 6130.0 nM 5.21
CHEMBL3116322 EC50 = 9880.0 nM 5.00
CHEMBL2216760 EC50 = 20860.0 nM 4.68
CHEMBL4173277 EC50 = 26700.0 nM 4.57
CHEMBL3116325 EC50 = 37000.0 nM 4.43
CHEMBL4159198 EC50 = 49800.0 nM 4.30