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Assay Detail

CHEMBL5360233

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 incubated for 18 hrs by QUANTI-Blue reagent based SEAP reporter assay
29
Total Activities
29
Compounds Tested
2
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

Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.
Poudel YB, He L, Cox M, Zhang Q, Johnson WL, Cong Q, Cheng H, Chowdari NS, Tarby C, Donnell AF, Broekema M, O'Malley DP, Zhang Y, A M Subbaiah M, Kumar BV, Subramani L, Wang B, Li YX, Sivaprakasam P, Critton D, Mulligan D, Sandhu B, Xie C, Ramakrishnan R, Nagar J, Dudhgaonkar S, Oderinde MS, Murtaza A, Schieven GL, Mathur A, Gavai AV, Vite G, Gangwar S.
ACS Med Chem Lett (2024) 15 : 181 -188
PubMed 38352830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.87 8.70
IC50 10 6.98 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433689 1 8.85
CHEMBL5429027 1 8.70
CHEMBL5419663 1 7.92
CHEMBL5407132 1 7.82
CHEMBL5431826 1 7.64
CHEMBL5418486 1 7.62
CHEMBL5434111 1 7.36
CHEMBL5399638 1 7.36
CHEMBL5416423 1 7.27
CHEMBL5439307 1 7.10
CHEMBL5409254 1 7.01
CHEMBL5440967 1 6.85
CHEMBL5401895 1 6.80
CHEMBL5437820 1 6.71
CHEMBL5425931 1 6.69
CHEMBL5435487 1 6.53
CHEMBL5398234 1 6.52
CHEMBL5397470 1 6.49
CHEMBL5397705 1 6.48
CHEMBL5438543 1 6.30
CHEMBL5414135 1 6.19
CHEMBL5416960 1 6.09
CHEMBL5436496 1 6.07
CHEMBL5400673 1 6.00
CHEMBL5439590 1 5.76
CHEMBL1085742 1 5.40
CHEMBL5400451 1 -
CHEMBL5416348 1 -
CHEMBL5405413 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433689 IC50 = 1.4 nM 8.85
CHEMBL5429027 EC50 = 2.0 nM 8.70
CHEMBL5419663 IC50 = 12.0 nM 7.92
CHEMBL5407132 EC50 = 15.0 nM 7.82
CHEMBL5431826 EC50 = 23.0 nM 7.64
CHEMBL5418486 EC50 = 24.0 nM 7.62
CHEMBL5434111 EC50 = 44.0 nM 7.36
CHEMBL5399638 EC50 = 44.0 nM 7.36
CHEMBL5416423 IC50 = 53.7 nM 7.27
CHEMBL5439307 EC50 = 79.0 nM 7.10
CHEMBL5409254 EC50 = 97.0 nM 7.01
CHEMBL5440967 EC50 = 140.0 nM 6.85
CHEMBL5401895 EC50 = 159.0 nM 6.80
CHEMBL5437820 IC50 = 197.0 nM 6.71
CHEMBL5425931 EC50 = 204.0 nM 6.69
CHEMBL5435487 EC50 = 293.0 nM 6.53
CHEMBL5398234 IC50 = 302.0 nM 6.52
CHEMBL5397470 EC50 = 321.0 nM 6.49
CHEMBL5397705 IC50 = 333.0 nM 6.48
CHEMBL5438543 EC50 = 495.0 nM 6.30
CHEMBL5414135 EC50 = 644.0 nM 6.19
CHEMBL5416960 EC50 = 807.0 nM 6.09
CHEMBL5436496 IC50 = 849.0 nM 6.07
CHEMBL5400673 IC50 = 1003.0 nM 6.00
CHEMBL5439590 EC50 = 1728.0 nM 5.76
CHEMBL1085742 EC50 = 4000.0 nM 5.40
CHEMBL5400451 IC50 > 5000.0 nM -
CHEMBL5416348 IC50 > 5000.0 nM -
CHEMBL5405413 EC50 > 5000.0 nM -