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Assay Detail

CHEMBL1103537

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

Functional
Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay
16
Total Activities
16
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

Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept.
Kurimoto A, Hashimoto K, Nakamura T, Norimura K, Ogita H, Takaku H, Bonnert R, McInally T, Wada H, Isobe Y.
J Med Chem (2010) 53 : 2964 -2972
PubMed 20232824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.03 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1092654 1 8.09
CHEMBL1089225 1 7.99
CHEMBL1093466 1 7.59
CHEMBL1089224 1 7.30
CHEMBL1089863 1 7.29
CHEMBL150961 1 7.20
CHEMBL1090529 1 7.14
CHEMBL1089226 1 7.12
CHEMBL1089548 1 7.06
CHEMBL1092655 1 6.97
CHEMBL1093467 1 6.73
CHEMBL383322 RESIQUIMOD 2.0 1 6.58
CHEMBL1089517 1 6.50
CHEMBL210884 1 6.40
CHEMBL1089220 1 6.33
CHEMBL1089862 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1092654 EC50 = 8.1 nM 8.09
CHEMBL1089225 EC50 = 10.3 nM 7.99
CHEMBL1093466 EC50 = 25.7 nM 7.59
CHEMBL1089224 EC50 = 50.1 nM 7.30
CHEMBL1089863 EC50 = 51.5 nM 7.29
CHEMBL150961 EC50 = 63.7 nM 7.20
CHEMBL1090529 EC50 = 72.9 nM 7.14
CHEMBL1089226 EC50 = 75.0 nM 7.12
CHEMBL1089548 EC50 = 87.5 nM 7.06
CHEMBL1092655 EC50 = 108.0 nM 6.97
CHEMBL1093467 EC50 = 187.9 nM 6.73
CHEMBL383322 RESIQUIMOD EC50 = 260.1 nM 6.58
CHEMBL1089517 EC50 = 312.3 nM 6.50
CHEMBL210884 EC50 = 399.4 nM 6.40
CHEMBL1089220 EC50 = 466.8 nM 6.33
CHEMBL1089862 EC50 = 609.1 nM 6.21