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Assay Detail

CHEMBL5149150

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

Binding
Agonist activity at TLR1/TLR2 in wild type C57BL/6J mouse macrophages assessed as stimulation of TNF alpha release measured for 4 hrs by ELISA based assay
94
Total Activities
94
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Macrophage
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Toll-like receptor 1/2 (CHEMBL3885644)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response.
Yang MH, Russell JL, Mifune Y, Wang Y, Shi H, Moresco EMY, Siegwart DJ, Beutler B, Boger DL.
J Med Chem (2022) 65 : 9230 -9252
PubMed 35767437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 94 7.80 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5205616 1 9.22
CHEMBL5195088 1 9.17
CHEMBL5191001 1 9.17
CHEMBL5196750 1 9.15
CHEMBL5179644 1 9.12
CHEMBL5181631 1 9.12
CHEMBL5183964 1 9.07
CHEMBL5181859 1 9.00
CHEMBL5192641 1 8.96
CHEMBL5199615 1 8.92
CHEMBL4472879 1 8.89
CHEMBL5179849 1 8.89
CHEMBL5190772 1 8.85
CHEMBL5203424 1 8.82
CHEMBL5169958 1 8.74
CHEMBL5184916 1 8.70
CHEMBL5169846 1 8.68
CHEMBL5191273 1 8.68
CHEMBL5206742 1 8.60
CHEMBL5201759 1 8.59
CHEMBL5170841 1 8.59
CHEMBL5172228 1 8.55
CHEMBL5198565 1 8.47
CHEMBL5180856 1 8.47
CHEMBL5203059 1 8.46
CHEMBL5188254 1 8.43
CHEMBL5169343 1 8.35
CHEMBL5202312 1 8.33
CHEMBL5208333 1 8.31
CHEMBL5174119 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5205616 EC50 = 0.6 nM 9.22
CHEMBL5195088 EC50 = 0.67 nM 9.17
CHEMBL5191001 EC50 = 0.67 nM 9.17
CHEMBL5196750 EC50 = 0.7 nM 9.15
CHEMBL5179644 EC50 = 0.75 nM 9.12
CHEMBL5181631 EC50 = 0.75 nM 9.12
CHEMBL5183964 EC50 = 0.85 nM 9.07
CHEMBL5181859 EC50 = 1.0 nM 9.00
CHEMBL5192641 EC50 = 1.1 nM 8.96
CHEMBL5199615 EC50 = 1.2 nM 8.92
CHEMBL4472879 EC50 = 1.3 nM 8.89
CHEMBL5179849 EC50 = 1.3 nM 8.89
CHEMBL5190772 EC50 = 1.4 nM 8.85
CHEMBL5203424 EC50 = 1.5 nM 8.82
CHEMBL5169958 EC50 = 1.8 nM 8.74
CHEMBL5184916 EC50 = 2.0 nM 8.70
CHEMBL5169846 EC50 = 2.1 nM 8.68
CHEMBL5191273 EC50 = 2.1 nM 8.68
CHEMBL5206742 EC50 = 2.5 nM 8.60
CHEMBL5201759 EC50 = 2.6 nM 8.59
CHEMBL5170841 EC50 = 2.6 nM 8.59
CHEMBL5172228 EC50 = 2.8 nM 8.55
CHEMBL5198565 EC50 = 3.4 nM 8.47
CHEMBL5180856 EC50 = 3.4 nM 8.47
CHEMBL5203059 EC50 = 3.5 nM 8.46
CHEMBL5188254 EC50 = 3.7 nM 8.43
CHEMBL5169343 EC50 = 4.5 nM 8.35
CHEMBL5202312 EC50 = 4.7 nM 8.33
CHEMBL5208333 EC50 = 4.9 nM 8.31
CHEMBL5174119 EC50 = 5.0 nM 8.30
CHEMBL5207112 EC50 = 5.0 nM 8.30
CHEMBL5186180 EC50 = 5.0 nM 8.30
CHEMBL5205724 EC50 = 5.0 nM 8.30
CHEMBL5187007 EC50 = 5.0 nM 8.30
CHEMBL5208283 EC50 = 5.3 nM 8.28
CHEMBL5205713 EC50 = 5.3 nM 8.28
CHEMBL5193298 EC50 = 6.0 nM 8.22
CHEMBL5205549 EC50 = 6.0 nM 8.22
CHEMBL5196411 EC50 = 6.0 nM 8.22
CHEMBL5191877 EC50 = 6.2 nM 8.21
CHEMBL5185241 EC50 = 6.3 nM 8.20
CHEMBL5193367 EC50 = 6.7 nM 8.17
CHEMBL5205005 EC50 = 7.0 nM 8.15
CHEMBL5197635 EC50 = 9.2 nM 8.04
CHEMBL5181846 EC50 = 10.0 nM 8.00
CHEMBL5188206 EC50 = 10.0 nM 8.00
CHEMBL5182713 EC50 = 16.0 nM 7.80
CHEMBL5176430 EC50 = 17.0 nM 7.77
CHEMBL5201813 EC50 = 17.0 nM 7.77
CHEMBL5190146 EC50 = 19.0 nM 7.72