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Assay Detail

CHEMBL859867

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

Binding
Average Binding Constant for EGFR; NA=Not Active at 10 uM
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A small molecule-kinase interaction map for clinical kinase inhibitors.
Fabian MA, Biggs WH, Treiber DK, Atteridge CE, Azimioara MD, Benedetti MG, Carter TA, Ciceri P, Edeen PT, Floyd M, Ford JM, Galvin M, Gerlach JL, Grotzfeld RM, Herrgard S, Insko DE, Insko MA, Lai AG, Lélias JM, Mehta SA, Milanov ZV, Velasco AM, Wodicka LM, Patel HK, Zarrinkar PP, Lockhart DJ.
Nat Biotechnol (2005) 23 : 329 -336
PubMed 15711537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 20 7.72 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL607707 PELITINIB 2.0 1 9.00
CHEMBL31965 CANERTINIB 3.0 1 8.85
CHEMBL553 ERLOTINIB 4.0 1 8.85
CHEMBL939 GEFITINIB 4.0 1 8.74
CHEMBL554 LAPATINIB 4.0 1 8.26
CHEMBL24828 VANDETANIB 4.0 1 7.77
CHEMBL388978 STAUROSPORINE 1 7.16
CHEMBL10 SB-203580 1 5.54
CHEMBL278041 SB-202190 1 5.34
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL101253 VATALANIB 3.0 1 -
CHEMBL1336 SORAFENIB 4.0 1 -
CHEMBL941 IMATINIB 4.0 1 -
CHEMBL1725279 SP-600125 1 -
CHEMBL103667 DORAMAPIMOD 2.0 1 -
CHEMBL119385 NEFLAMAPIMOD 2.0 1 -
CHEMBL535 SUNITINIB 4.0 1 -
CHEMBL14762 SELICICLIB 2.0 1 -
CHEMBL428690 ALVOCIDIB 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL607707 PELITINIB Kd = 1.0 nM 9.00
CHEMBL31965 CANERTINIB Kd = 1.4 nM 8.85
CHEMBL553 ERLOTINIB Kd = 1.4 nM 8.85
CHEMBL939 GEFITINIB Kd = 1.8 nM 8.74
CHEMBL554 LAPATINIB Kd = 5.5 nM 8.26
CHEMBL24828 VANDETANIB Kd = 17.0 nM 7.77
CHEMBL388978 STAUROSPORINE Kd = 70.0 nM 7.16
CHEMBL10 SB-203580 Kd = 2900.0 nM 5.54
CHEMBL278041 SB-202190 Kd = 4600.0 nM 5.34
CHEMBL124660 TANDUTINIB Kd - -
CHEMBL91829 RUBOXISTAURIN Kd - -
CHEMBL101253 VATALANIB Kd - -
CHEMBL1336 SORAFENIB Kd - -
CHEMBL941 IMATINIB Kd - -
CHEMBL1725279 SP-600125 Kd - -
CHEMBL103667 DORAMAPIMOD Kd - -
CHEMBL119385 NEFLAMAPIMOD Kd - -
CHEMBL535 SUNITINIB Kd - -
CHEMBL14762 SELICICLIB Kd - -
CHEMBL428690 ALVOCIDIB Kd - -