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Assay Detail

CHEMBL1926410

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

Functional
Agonist activity at human TLR2 expressed in HEK293 cells assessed as NF-kappaB induction measured soluble alkaline phosphatase after 12 hrs by spectrophotometric analysis
22
Total Activities
22
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 2 (CHEMBL4163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships in toll-like receptor 2-agonists leading to simplified monoacyl lipopeptides.
Agnihotri G, Crall BM, Lewis TC, Day TP, Balakrishna R, Warshakoon HJ, Malladi SS, David SA.
J Med Chem (2011) 54 : 8148 -8160
PubMed 22007676 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.85 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1923557 1 9.59
CHEMBL1923536 1 9.35
CHEMBL1923541 1 9.25
CHEMBL1923538 1 9.06
CHEMBL1923537 1 9.00
CHEMBL1923542 1 8.83
CHEMBL1923545 1 8.81
CHEMBL1923548 1 8.73
CHEMBL1923547 1 8.71
CHEMBL1923544 1 8.68
CHEMBL1923546 1 8.49
CHEMBL1923549 1 8.35
CHEMBL1923540 1 8.19
CHEMBL1923543 1 -
CHEMBL1923550 1 -
CHEMBL1923551 1 -
CHEMBL1923552 1 -
CHEMBL1923553 1 -
CHEMBL1923554 1 -
CHEMBL1923555 1 -
CHEMBL1923556 1 -
CHEMBL1923539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1923557 EC50 = 0.26 nM 9.59
CHEMBL1923536 EC50 = 0.45 nM 9.35
CHEMBL1923541 EC50 = 0.56 nM 9.25
CHEMBL1923538 EC50 = 0.87 nM 9.06
CHEMBL1923537 EC50 = 1.0 nM 9.00
CHEMBL1923542 EC50 = 1.47 nM 8.83
CHEMBL1923545 EC50 = 1.55 nM 8.81
CHEMBL1923548 EC50 = 1.86 nM 8.73
CHEMBL1923547 EC50 = 1.95 nM 8.71
CHEMBL1923544 EC50 = 2.11 nM 8.68
CHEMBL1923546 EC50 = 3.23 nM 8.49
CHEMBL1923549 EC50 = 4.44 nM 8.35
CHEMBL1923540 EC50 = 6.48 nM 8.19
CHEMBL1923543 EC50 > 1000.0 nM -
CHEMBL1923550 EC50 > 1000.0 nM -
CHEMBL1923551 EC50 > 1000.0 nM -
CHEMBL1923552 EC50 > 1000.0 nM -
CHEMBL1923553 EC50 > 1000.0 nM -
CHEMBL1923554 EC50 > 1000.0 nM -
CHEMBL1923555 EC50 > 1000.0 nM -
CHEMBL1923556 EC50 > 1000.0 nM -
CHEMBL1923539 EC50 > 1000.0 nM -