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Assay Detail

CHEMBL3881373

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

Binding
Antagonist activity at TLR1/2 in mouse RAW264.7 cells assessed as inhibition of Pam3CSK4-induced receptor activation by measuring NO production after 24 hrs
28
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type RAW264.7
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Antagonists of the toll-like receptor 1/2 complex
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.39 6.24
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3935646 2 6.24
CHEMBL3985620 1 6.14
CHEMBL3968633 1 6.00
CHEMBL3914204 1 5.90
CHEMBL3973420 1 5.87
CHEMBL3940598 1 5.87
CHEMBL3950566 1 5.85
CHEMBL3964783 1 5.65
CHEMBL1485442 1 5.63
CHEMBL66953 PURPUROGALLIN 1 5.61
CHEMBL3953549 1 5.61
CHEMBL3937503 1 5.55
CHEMBL3932936 1 5.55
CHEMBL3915397 1 5.51
CHEMBL3966770 1 5.50
CHEMBL3911544 1 5.49
CHEMBL3909287 1 5.39
CHEMBL3966320 1 5.32
CHEMBL3916747 1 5.32
CHEMBL1556914 METHYL 7-DESHYDROXYPYROGALLIN-4-CARBOXYLATE 1 5.04
CHEMBL1508229 1 4.93
CHEMBL3964988 1 4.83
CHEMBL559337 7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID 1 4.78
CHEMBL3912810 1 4.67
CHEMBL3902323 1 4.64
CHEMBL134871 1 4.40
CHEMBL3966006 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3935646 IC50 = 580.0 nM 6.24
CHEMBL3985620 IC50 = 720.0 nM 6.14
CHEMBL3968633 IC50 = 1010.0 nM 6.00
CHEMBL3914204 IC50 = 1260.0 nM 5.90
CHEMBL3940598 IC50 = 1360.0 nM 5.87
CHEMBL3973420 IC50 = 1360.0 nM 5.87
CHEMBL3950566 IC50 = 1420.0 nM 5.85
CHEMBL3964783 IC50 = 2250.0 nM 5.65
CHEMBL1485442 IC50 = 2350.0 nM 5.63
CHEMBL66953 PURPUROGALLIN IC50 = 2450.0 nM 5.61
CHEMBL3953549 IC50 = 2470.0 nM 5.61
CHEMBL3932936 IC50 = 2830.0 nM 5.55
CHEMBL3937503 IC50 = 2830.0 nM 5.55
CHEMBL3915397 IC50 = 3110.0 nM 5.51
CHEMBL3966770 IC50 = 3130.0 nM 5.50
CHEMBL3911544 IC50 = 3240.0 nM 5.49
CHEMBL3909287 IC50 = 4110.0 nM 5.39
CHEMBL3916747 IC50 = 4830.0 nM 5.32
CHEMBL3966320 IC50 = 4830.0 nM 5.32
CHEMBL1556914 METHYL 7-DESHYDROXYPYROGALLIN-4-CARBOXYLATE IC50 = 9010.0 nM 5.04
CHEMBL1508229 IC50 = 11730.0 nM 4.93
CHEMBL3964988 IC50 = 14820.0 nM 4.83
CHEMBL559337 7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID IC50 = 16490.0 nM 4.78
CHEMBL3912810 IC50 = 21510.0 nM 4.67
CHEMBL3902323 IC50 = 22740.0 nM 4.64
CHEMBL134871 IC50 = 39910.0 nM 4.40
CHEMBL3966006 IC50 = 74580.0 nM 4.13
CHEMBL3935646 Inhibition - % -