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Assay Detail

CHEMBL923921

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

Binding
Inhibition of human recombinant EGFR by fluorescence polarization assay
24
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Pannala M, Kher S, Wilson N, Gaudette J, Sircar I, Zhang SH, Bakhirev A, Yang G, Yuen P, Gorcsan F, Sakurai N, Barbosa M, Cheng JF.
Bioorg Med Chem Lett (2007) 17 : 5978 -5982
PubMed 17827009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.12 8.52
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248393 1 8.52
CHEMBL248392 1 8.08
CHEMBL248044 1 7.62
CHEMBL246419 1 7.44
CHEMBL245800 1 7.40
CHEMBL247196 1 7.36
CHEMBL248425 1 7.28
CHEMBL248221 1 7.28
CHEMBL401251 1 7.22
CHEMBL401054 1 7.19
CHEMBL248222 1 7.17
CHEMBL399438 1 7.10
CHEMBL245996 1 7.10
CHEMBL248220 1 6.92
CHEMBL248045 1 6.75
CHEMBL248391 1 6.66
CHEMBL400742 1 6.66
CHEMBL245799 1 6.47
CHEMBL245798 1 6.44
CHEMBL401644 1 6.44
CHEMBL247024 1 6.40
CHEMBL247197 1 -
CHEMBL399137 1 -
CHEMBL400194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248393 Ki = 3.0 nM 8.52
CHEMBL248392 Ki = 8.4 nM 8.08
CHEMBL248044 Ki = 24.0 nM 7.62
CHEMBL246419 Ki = 36.0 nM 7.44
CHEMBL245800 Ki = 40.0 nM 7.40
CHEMBL247196 Ki = 44.0 nM 7.36
CHEMBL248425 Ki = 52.0 nM 7.28
CHEMBL248221 Ki = 52.0 nM 7.28
CHEMBL401251 Ki = 60.0 nM 7.22
CHEMBL401054 Ki = 64.0 nM 7.19
CHEMBL248222 Ki = 68.0 nM 7.17
CHEMBL399438 Ki = 80.0 nM 7.10
CHEMBL245996 Ki = 80.0 nM 7.10
CHEMBL248220 Ki = 120.0 nM 6.92
CHEMBL248045 Ki = 180.0 nM 6.75
CHEMBL248391 Ki = 220.0 nM 6.66
CHEMBL400742 Ki = 220.0 nM 6.66
CHEMBL245799 Ki = 340.0 nM 6.47
CHEMBL245798 Ki = 360.0 nM 6.44
CHEMBL401644 Ki = 360.0 nM 6.44
CHEMBL247024 Ki = 400.0 nM 6.40
CHEMBL247197 Activity - -
CHEMBL399137 Activity - -
CHEMBL400194 Activity - -