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Assay Detail

CHEMBL4718820

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

Binding
Inhibition of human EGFR using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma33P]ATP by radiometric HotSpot assay
ChEMBL ↗
46
Total Activities
46
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

Balancing potency, metabolic stability and permeability in pyrrolopyrimidine-based EGFR inhibitors.
Han J,Henriksen S,Nørsett KG,Sundby E,Hoff BH
Eur J Med Chem (2016) 124 : 583 -607
PubMed 27614407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 9.25 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4787951 — — 1 10.00
CHEMBL4784258 — — 1 10.00
CHEMBL4759003 — — 1 10.00
CHEMBL4748367 — — 1 10.00
CHEMBL4742081 — — 1 10.00
CHEMBL4778248 — — 1 10.00
CHEMBL4760328 — — 1 10.00
CHEMBL4776396 — — 1 9.70
CHEMBL4748320 — — 1 9.52
CHEMBL4740573 — — 1 9.52
CHEMBL4787816 — — 1 9.52
CHEMBL4743998 — — 1 9.52
CHEMBL4785569 — — 1 9.52
CHEMBL4793053 — — 1 9.40
CHEMBL553 ERLOTINIB 4.0 1 9.40
CHEMBL4795296 — — 1 9.40
CHEMBL4757806 — — 1 9.40
CHEMBL4784777 — — 1 9.40
CHEMBL4783569 — — 1 9.40
CHEMBL4763315 — — 1 9.30
CHEMBL4792577 — — 1 9.30
CHEMBL4786776 — — 1 9.30
CHEMBL4776751 — — 1 9.30
CHEMBL4170121 — — 1 9.22
CHEMBL4746770 — — 1 9.22
CHEMBL4789027 — — 1 9.22
CHEMBL4741922 — — 1 9.22
CHEMBL4749862 — — 1 9.22
CHEMBL4759127 — — 1 9.15
CHEMBL4751641 — — 1 9.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4787951 — IC50 = 0.1 nM 10.00
CHEMBL4784258 — IC50 = 0.1 nM 10.00
CHEMBL4759003 — IC50 = 0.1 nM 10.00
CHEMBL4748367 — IC50 = 0.1 nM 10.00
CHEMBL4742081 — IC50 = 0.1 nM 10.00
CHEMBL4778248 — IC50 = 0.1 nM 10.00
CHEMBL4760328 — IC50 = 0.1 nM 10.00
CHEMBL4776396 — IC50 = 0.2 nM 9.70
CHEMBL4748320 — IC50 = 0.3 nM 9.52
CHEMBL4740573 — IC50 = 0.3 nM 9.52
CHEMBL4787816 — IC50 = 0.3 nM 9.52
CHEMBL4743998 — IC50 = 0.3 nM 9.52
CHEMBL4785569 — IC50 = 0.3 nM 9.52
CHEMBL4783569 — IC50 = 0.4 nM 9.40
CHEMBL553 ERLOTINIB IC50 = 0.4 nM 9.40
CHEMBL4795296 — IC50 = 0.4 nM 9.40
CHEMBL4757806 — IC50 = 0.4 nM 9.40
CHEMBL4793053 — IC50 = 0.4 nM 9.40
CHEMBL4784777 — IC50 = 0.4 nM 9.40
CHEMBL4763315 — IC50 = 0.5 nM 9.30
CHEMBL4792577 — IC50 = 0.5 nM 9.30
CHEMBL4786776 — IC50 = 0.5 nM 9.30
CHEMBL4776751 — IC50 = 0.5 nM 9.30
CHEMBL4170121 — IC50 = 0.6 nM 9.22
CHEMBL4749862 — IC50 = 0.6 nM 9.22
CHEMBL4741922 — IC50 = 0.6 nM 9.22
CHEMBL4746770 — IC50 = 0.6 nM 9.22
CHEMBL4789027 — IC50 = 0.6 nM 9.22
CHEMBL4759127 — IC50 = 0.7 nM 9.15
CHEMBL4751641 — IC50 = 0.7 nM 9.15
CHEMBL4778894 — IC50 = 0.7 nM 9.15
CHEMBL4744798 — IC50 = 0.7 nM 9.15
CHEMBL4746697 — IC50 = 0.8 nM 9.10
CHEMBL4791195 — IC50 = 0.8 nM 9.10
CHEMBL4740295 — IC50 = 0.8 nM 9.10
CHEMBL4780286 — IC50 = 0.8 nM 9.10
CHEMBL4764993 — IC50 = 0.8 nM 9.10
CHEMBL4779711 — IC50 = 1.1 nM 8.96
CHEMBL4749064 — IC50 = 1.2 nM 8.92
CHEMBL4794073 — IC50 = 1.3 nM 8.89
CHEMBL4776056 — IC50 = 1.4 nM 8.85
CHEMBL4748149 — IC50 = 1.6 nM 8.80
CHEMBL4780965 — IC50 = 2.0 nM 8.70
CHEMBL4789312 — IC50 = 2.2 nM 8.66
CHEMBL4800697 — IC50 = 4.3 nM 8.37
CHEMBL4753008 — IC50 = 900.0 nM 6.05