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Assay Detail

CHEMBL1243977

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

Binding
Inhibition of recombinant EGFR by radioactive phosphotransfer assay in presence of 10 uM ATP
209
Total Activities
209
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA.
Nat Chem Biol (2008) 4 : 691 -699
PubMed 18849971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 209 5.35 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 7.70
CHEMBL1241487 1 7.48
CHEMBL1241676 1 7.17
CHEMBL1241581 1 7.08
CHEMBL1242664 1 7.07
CHEMBL1242662 1 7.06
CHEMBL1241484 1 6.80
CHEMBL1241481 1 6.77
CHEMBL1242294 1 6.75
CHEMBL1242852 1 6.75
CHEMBL1242476 1 6.68
CHEMBL1242574 1 6.66
CHEMBL1242376 1 6.63
CHEMBL1242285 1 6.60
CHEMBL1081312 1 6.58
CHEMBL1242202 1 6.57
CHEMBL1242568 1 6.50
CHEMBL1242287 1 6.49
CHEMBL1242656 1 6.44
CHEMBL1242293 1 6.42
CHEMBL1234815 1 6.41
CHEMBL1242853 1 6.41
CHEMBL1242201 1 6.36
CHEMBL1242755 1 6.27
CHEMBL1242385 1 6.27
CHEMBL1241578 1 6.26
CHEMBL1242198 1 6.24
CHEMBL1242115 1 6.24
CHEMBL1242475 1 6.24
CHEMBL1241491 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 20.0 nM 7.70
CHEMBL1241487 IC50 = 33.0 nM 7.48
CHEMBL1241676 IC50 = 67.0 nM 7.17
CHEMBL1241581 IC50 = 84.0 nM 7.08
CHEMBL1242664 IC50 = 85.0 nM 7.07
CHEMBL1242662 IC50 = 88.0 nM 7.06
CHEMBL1241484 IC50 = 158.0 nM 6.80
CHEMBL1241481 IC50 = 170.0 nM 6.77
CHEMBL1242852 IC50 = 179.0 nM 6.75
CHEMBL1242294 IC50 = 176.0 nM 6.75
CHEMBL1242476 IC50 = 207.0 nM 6.68
CHEMBL1242574 IC50 = 220.0 nM 6.66
CHEMBL1242376 IC50 = 236.0 nM 6.63
CHEMBL1242285 IC50 = 249.0 nM 6.60
CHEMBL1081312 IC50 = 260.0 nM 6.58
CHEMBL1242202 IC50 = 270.0 nM 6.57
CHEMBL1242568 IC50 = 318.0 nM 6.50
CHEMBL1242287 IC50 = 324.0 nM 6.49
CHEMBL1242656 IC50 = 366.0 nM 6.44
CHEMBL1242293 IC50 = 380.0 nM 6.42
CHEMBL1242853 IC50 = 391.0 nM 6.41
CHEMBL1234815 IC50 = 388.0 nM 6.41
CHEMBL1242201 IC50 = 437.0 nM 6.36
CHEMBL1242385 IC50 = 539.0 nM 6.27
CHEMBL1242755 IC50 = 540.0 nM 6.27
CHEMBL1241578 IC50 = 550.0 nM 6.26
CHEMBL1242198 IC50 = 576.0 nM 6.24
CHEMBL1242475 IC50 = 571.0 nM 6.24
CHEMBL1242115 IC50 = 579.0 nM 6.24
CHEMBL1241491 IC50 = 575.0 nM 6.24
CHEMBL1233882 IC50 = 610.0 nM 6.21
CHEMBL1242666 IC50 = 638.0 nM 6.20
CHEMBL1242026 IC50 = 663.0 nM 6.18
CHEMBL1242295 IC50 = 734.0 nM 6.13
CHEMBL1242289 IC50 = 768.0 nM 6.12
CHEMBL1242199 IC50 = 751.0 nM 6.12
CHEMBL1242572 IC50 = 760.0 nM 6.12
CHEMBL1242750 IC50 = 775.0 nM 6.11
CHEMBL1241241 IC50 = 922.0 nM 6.04
CHEMBL1242112 IC50 = 908.0 nM 6.04
CHEMBL1241586 IC50 = 937.0 nM 6.03
CHEMBL1230790 IC50 = 954.0 nM 6.02
CHEMBL1242384 IC50 = 955.0 nM 6.02
CHEMBL1242024 IC50 = 954.0 nM 6.02
CHEMBL1241490 IC50 = 964.0 nM 6.02
CHEMBL1242754 IC50 = 1000.0 nM 6.00
CHEMBL1241945 IC50 = 1040.0 nM 5.98
CHEMBL1242386 IC50 = 1100.0 nM 5.96
CHEMBL1241580 IC50 = 1150.0 nM 5.94
CHEMBL1242659 IC50 = 1160.0 nM 5.94