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Assay Detail

CHEMBL5360423

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

Binding
Agonist activity at human TLR7 in HEK-Blue hTLR7 cells harboring SEAP reporter transgene incubated for 18 hrs by quanti-blue reagent based assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-Blue hTLR7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.
He L, Zhang MY, Cox M, Zhang Q, Donnell AF, Zhang Y, Tarby C, Gill P, Subbaiah MAM, Ramar T, Reddy M, Puttapaka V, Li YX, Sivaprakasam P, Critton D, Mulligan D, Xie C, Ramakrishnan R, Nagar J, Dudhgaonkar S, Murtaza A, Oderinde MS, Schieven GL, Mathur A, Gavai AV, Vite G, Gangwar S, Poudel YB.
ACS Med Chem Lett (2024) 15 : 189 -196
PubMed 38352849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 7.03 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5404211 1 7.92
CHEMBL5419663 1 7.92
CHEMBL5435264 1 7.89
CHEMBL5417891 1 7.89
CHEMBL5427289 1 7.85
CHEMBL5426019 1 7.75
CHEMBL5407698 1 7.68
CHEMBL5414529 1 7.32
CHEMBL5418809 1 7.31
CHEMBL5403684 1 7.25
CHEMBL5413224 1 7.24
CHEMBL5411647 1 7.09
CHEMBL5398842 1 7.08
CHEMBL5427884 1 7.06
CHEMBL5417342 1 6.88
CHEMBL5427789 1 6.87
CHEMBL5430110 1 6.84
CHEMBL5419694 1 6.79
CHEMBL5427518 1 6.57
CHEMBL5400486 1 6.50
CHEMBL5434082 1 6.43
CHEMBL5413300 1 6.43
CHEMBL5419165 1 6.34
CHEMBL5424102 1 6.26
CHEMBL5414156 1 6.24
CHEMBL5427987 1 6.17
CHEMBL5420635 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5404211 EC50 = 12.0 nM 7.92
CHEMBL5419663 EC50 = 12.0 nM 7.92
CHEMBL5435264 EC50 = 13.0 nM 7.89
CHEMBL5417891 EC50 = 13.0 nM 7.89
CHEMBL5427289 EC50 = 14.0 nM 7.85
CHEMBL5426019 EC50 = 18.0 nM 7.75
CHEMBL5407698 EC50 = 21.0 nM 7.68
CHEMBL5414529 EC50 = 48.0 nM 7.32
CHEMBL5418809 EC50 = 49.0 nM 7.31
CHEMBL5403684 EC50 = 56.0 nM 7.25
CHEMBL5413224 EC50 = 58.0 nM 7.24
CHEMBL5411647 EC50 = 82.0 nM 7.09
CHEMBL5398842 EC50 = 84.0 nM 7.08
CHEMBL5427884 EC50 = 87.0 nM 7.06
CHEMBL5417342 EC50 = 133.0 nM 6.88
CHEMBL5427789 EC50 = 134.0 nM 6.87
CHEMBL5430110 EC50 = 145.0 nM 6.84
CHEMBL5419694 EC50 = 163.0 nM 6.79
CHEMBL5427518 EC50 = 272.0 nM 6.57
CHEMBL5400486 EC50 = 315.0 nM 6.50
CHEMBL5434082 EC50 = 370.0 nM 6.43
CHEMBL5413300 EC50 = 370.0 nM 6.43
CHEMBL5419165 EC50 = 461.0 nM 6.34
CHEMBL5424102 EC50 = 549.0 nM 6.26
CHEMBL5414156 EC50 = 572.0 nM 6.24
CHEMBL5427987 EC50 = 668.0 nM 6.17
CHEMBL5420635 EC50 = 780.0 nM 6.11