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Assay Detail

CHEMBL3737823

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

Binding
Inhibition of human EGFR T790M/L858R double mutant using Fl-EEPLYWSFPAKKK-CONH2 as substrate preincubated for 30 mins followed by addition of substrate measured after 30 mins by Morrison plot analysis
ChEMBL ↗
42
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, Lainchbury M, Malek S, Mann S, Merchant M, Mortara K, Purkey H, Schaefer G, Schmidt S, Seward E, Sideris S, Shao L, Wang S, Yeap K, Yen I, Yu C, Heffron TP.
J Med Chem (2015) 58 : 8877 -8895
PubMed 26455919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.42 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3736121 — — 1 8.96
CHEMBL3734988 — — 1 8.60
CHEMBL3736183 — — 1 8.57
CHEMBL3734933 — — 1 8.37
CHEMBL3735474 — — 1 8.13
CHEMBL3734786 — — 1 8.02
CHEMBL3735958 — — 1 7.89
CHEMBL3735250 — — 3 7.85
CHEMBL3734934 — — 1 7.80
CHEMBL3735335 — — 1 7.75
CHEMBL3736508 — — 1 7.72
CHEMBL3734877 — — 1 7.72
CHEMBL3734825 — — 1 7.70
CHEMBL3735689 — — 1 7.66
CHEMBL3736395 — — 1 7.62
CHEMBL3736365 — — 1 7.57
CHEMBL3736430 — — 1 7.55
CHEMBL3735533 — — 1 7.47
CHEMBL3735782 — — 1 7.42
CHEMBL3354190 — — 1 7.40
CHEMBL3735740 — — 1 7.36
CHEMBL3736409 — — 1 7.32
CHEMBL3736191 — — 1 7.30
CHEMBL3736210 — — 1 7.28
CHEMBL3736181 — — 1 7.24
CHEMBL3735045 — — 1 7.19
CHEMBL3736254 — — 1 7.15
CHEMBL3735725 — — 1 7.12
CHEMBL3735848 — — 1 7.11
CHEMBL3736178 — — 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3736121 — Ki = 1.1 nM 8.96
CHEMBL3734988 — Ki = 2.5 nM 8.60
CHEMBL3736183 — Ki = 2.7 nM 8.57
CHEMBL3734933 — Ki = 4.3 nM 8.37
CHEMBL3735474 — Ki = 7.4 nM 8.13
CHEMBL3734786 — Ki = 9.5 nM 8.02
CHEMBL3735958 — Ki = 13.0 nM 7.89
CHEMBL3735250 — Ki = 14.0 nM 7.85
CHEMBL3734934 — Ki = 16.0 nM 7.80
CHEMBL3735250 — Ki = 17.0 nM 7.77
CHEMBL3735335 — Ki = 18.0 nM 7.75
CHEMBL3734877 — Ki = 19.0 nM 7.72
CHEMBL3736508 — Ki = 19.0 nM 7.72
CHEMBL3734825 — Ki = 20.0 nM 7.70
CHEMBL3735250 — Ki = 22.0 nM 7.66
CHEMBL3735689 — Ki = 22.0 nM 7.66
CHEMBL3736395 — Ki = 24.0 nM 7.62
CHEMBL3736365 — Ki = 27.0 nM 7.57
CHEMBL3736430 — Ki = 28.0 nM 7.55
CHEMBL3735533 — Ki = 34.0 nM 7.47
CHEMBL3735782 — Ki = 38.0 nM 7.42
CHEMBL3354190 — Ki = 40.0 nM 7.40
CHEMBL3735740 — Ki = 44.0 nM 7.36
CHEMBL3736409 — Ki = 48.0 nM 7.32
CHEMBL3736191 — Ki = 50.0 nM 7.30
CHEMBL3736210 — Ki = 52.0 nM 7.28
CHEMBL3736181 — Ki = 57.0 nM 7.24
CHEMBL3735045 — Ki = 64.0 nM 7.19
CHEMBL3736254 — Ki = 71.0 nM 7.15
CHEMBL3735725 — Ki = 76.0 nM 7.12
CHEMBL3735848 — Ki = 77.0 nM 7.11
CHEMBL3736178 — Ki = 87.0 nM 7.06
CHEMBL3735638 — Ki = 124.0 nM 6.91
CHEMBL3734928 — Ki = 149.0 nM 6.83
CHEMBL3735410 — Ki = 151.0 nM 6.82
CHEMBL3735892 — Ki = 196.0 nM 6.71
CHEMBL3735559 — Ki = 196.0 nM 6.71
CHEMBL3736094 — Ki = 201.0 nM 6.70
CHEMBL3735157 — Ki = 323.0 nM 6.49
CHEMBL3735952 — Ki = 329.0 nM 6.48
CHEMBL3735927 — Ki = 492.0 nM 6.31
CHEMBL3736480 — Ki = 658.0 nM 6.18