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Assay Detail

CHEMBL1120541

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

Functional
Agonist activity at human TLR7 expressed in NF-kappaB-stimulated HEK293 cells assessed as induction of secreted alkaline phosphatase expression by reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Structure-activity relationships in human toll-like receptor 7-active imidazoquinoline analogues.
Shukla NM, Malladi SS, Mutz CA, Balakrishna R, David SA.
J Med Chem (2010) 53 : 4450 -4465
PubMed 20481492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.23 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082983 1 8.07
CHEMBL1086473 1 7.23
CHEMBL1086474 1 7.04
CHEMBL1082642 1 6.68
CHEMBL1082399 1 6.58
CHEMBL1082982 1 6.42
CHEMBL1083637 1 6.33
CHEMBL1082376 1 6.32
CHEMBL1086143 1 6.19
CHEMBL1082307 1 6.14
CHEMBL1086372 1 6.08
CHEMBL1082336 1 6.06
CHEMBL1082304 1 6.02
CHEMBL1085742 1 5.70
CHEMBL1282 IMIQUIMOD 4.0 1 5.67
CHEMBL1083026 1 5.47
CHEMBL1082364 1 5.11
CHEMBL1084998 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082983 EC50 = 8.58 nM 8.07
CHEMBL1086473 EC50 = 59.1 nM 7.23
CHEMBL1086474 EC50 = 91.5 nM 7.04
CHEMBL1082642 EC50 = 209.0 nM 6.68
CHEMBL1082399 EC50 = 262.0 nM 6.58
CHEMBL1082982 EC50 = 385.0 nM 6.42
CHEMBL1083637 EC50 = 472.0 nM 6.33
CHEMBL1082376 EC50 = 479.0 nM 6.32
CHEMBL1086143 EC50 = 647.0 nM 6.19
CHEMBL1082307 EC50 = 723.0 nM 6.14
CHEMBL1086372 EC50 = 822.0 nM 6.08
CHEMBL1082336 EC50 = 873.0 nM 6.06
CHEMBL1082304 EC50 = 955.0 nM 6.02
CHEMBL1085742 EC50 = 2000.0 nM 5.70
CHEMBL1282 IMIQUIMOD EC50 = 2120.0 nM 5.67
CHEMBL1083026 EC50 = 3350.0 nM 5.47
CHEMBL1082364 EC50 = 7710.0 nM 5.11
CHEMBL1084998 EC50 = 8390.0 nM 5.08