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Assay Detail

CHEMBL3790707

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

ADMET
Reversible binding affinity to human wild type EGFR expressed in baculovirus by fluorometric analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC.
J Med Chem (2016) 59 : 2005 -2024
PubMed 26756222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.80 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786098 PF-06459988 2.0 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786098 PF-06459988 Ki = 1600.0 nM 5.80