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Assay Detail

CHEMBL3881964

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

Binding
Inhibition of N-terminal GST-fused human EGFR (His672 to Ala1210 residues) expressed in baculovirus expression system using biotinylated PTP1B at Tyr66 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by DELFIA
ChEMBL ↗
108
Total Activities
108
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

Multi-functional small molecules as anti-proliferative agents
(2008)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 108 7.02 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL598797 CUDC-101 1.0 1 8.62
CHEMBL598377 — — 1 8.51
CHEMBL553 ERLOTINIB 4.0 1 7.32
CHEMBL3906200 — — 1 7.00
CHEMBL3985004 — — 1 7.00
CHEMBL3914322 — — 1 7.00
CHEMBL3917105 — — 1 7.00
CHEMBL3898480 — — 1 7.00
CHEMBL3950023 — — 1 7.00
CHEMBL3914607 — — 1 7.00
CHEMBL596964 — — 1 7.00
CHEMBL3917951 — — 1 7.00
CHEMBL2309506 — — 1 7.00
CHEMBL3984008 — — 1 7.00
CHEMBL3924787 — — 1 7.00
CHEMBL3922068 — — 1 7.00
CHEMBL3975990 — — 1 7.00
CHEMBL3912598 — — 1 7.00
CHEMBL3979482 — — 1 7.00
CHEMBL3909214 — — 1 7.00
CHEMBL2309507 — — 1 7.00
CHEMBL3975710 — — 1 6.00
CHEMBL3910297 — — 1 6.00
CHEMBL599218 — — 1 6.00
CHEMBL3949197 — — 1 -
CHEMBL597551 — — 1 -
CHEMBL597752 — — 1 -
CHEMBL596736 — — 1 -
CHEMBL598163 — — 1 -
CHEMBL3896110 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL598797 CUDC-101 IC50 = 2.4 nM 8.62
CHEMBL598377 — IC50 = 3.1 nM 8.51
CHEMBL553 ERLOTINIB IC50 = 48.0 nM 7.32
CHEMBL3985004 — IC50 = 100.0 nM 7.00
CHEMBL3909214 — IC50 = 100.0 nM 7.00
CHEMBL3914322 — IC50 = 100.0 nM 7.00
CHEMBL3917105 — IC50 = 100.0 nM 7.00
CHEMBL3979482 — IC50 = 100.0 nM 7.00
CHEMBL3898480 — IC50 = 100.0 nM 7.00
CHEMBL3912598 — IC50 = 100.0 nM 7.00
CHEMBL3975990 — IC50 = 100.0 nM 7.00
CHEMBL3950023 — IC50 = 100.0 nM 7.00
CHEMBL3984008 — IC50 = 100.0 nM 7.00
CHEMBL3924787 — IC50 = 100.0 nM 7.00
CHEMBL3906200 — IC50 = 100.0 nM 7.00
CHEMBL3914607 — IC50 = 100.0 nM 7.00
CHEMBL596964 — IC50 = 100.0 nM 7.00
CHEMBL2309507 — IC50 = 100.0 nM 7.00
CHEMBL2309506 — IC50 = 100.0 nM 7.00
CHEMBL3922068 — IC50 = 100.0 nM 7.00
CHEMBL3917951 — IC50 = 100.0 nM 7.00
CHEMBL3910297 — IC50 = 1000.0 nM 6.00
CHEMBL3975710 — IC50 = 1000.0 nM 6.00
CHEMBL599218 — IC50 = 1000.0 nM 6.00
CHEMBL3984573 — IC50 <= 100.0 nM -
CHEMBL3928197 — IC50 <= 100.0 nM -
CHEMBL3938265 — IC50 <= 100.0 nM -
CHEMBL3956995 — IC50 <= 100.0 nM -
CHEMBL3916600 — IC50 <= 100.0 nM -
CHEMBL3971713 — IC50 >= 10000.0 nM -
CHEMBL3968968 — IC50 <= 100.0 nM -
CHEMBL3939306 — IC50 <= 100.0 nM -
CHEMBL3952709 — IC50 <= 100.0 nM -
CHEMBL3984055 — IC50 <= 100.0 nM -
CHEMBL3905131 — IC50 <= 100.0 nM -
CHEMBL3901236 — IC50 <= 100.0 nM -
CHEMBL3917670 — IC50 <= 100.0 nM -
CHEMBL3986286 — IC50 <= 100.0 nM -
CHEMBL3972249 — IC50 <= 100.0 nM -
CHEMBL3937516 — IC50 <= 100.0 nM -
CHEMBL3903506 — IC50 <= 100.0 nM -
CHEMBL3945421 — IC50 <= 100.0 nM -
CHEMBL3948072 — IC50 <= 100.0 nM -
CHEMBL3907491 — IC50 <= 100.0 nM -
CHEMBL3976389 — IC50 <= 100.0 nM -
CHEMBL3976961 — IC50 <= 100.0 nM -
CHEMBL3980430 — IC50 <= 100.0 nM -
CHEMBL3930003 — IC50 <= 100.0 nM -
CHEMBL598799 — IC50 <= 100.0 nM -
CHEMBL3935462 — IC50 <= 100.0 nM -