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Assay Detail

CHEMBL4367477

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

Binding
Inhibition of NOD2/TLR2 in human PBMC assessed as reduction in MDP/Pam2CSK4-induced TNFalpha production preincubated for 30 mins followed by MDP/Pam2CSK4 stimulation and measured after 6 hrs by immunoassay
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.
Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW.
J Med Chem (2019) 62 : 6482 -6494
PubMed 31265286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 1 - -
IC50 1 7.60 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3822577 2 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3822577 IC50 = 25.0 nM 7.60
CHEMBL3822577 Inhibition - % -