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Assay Detail

CHEMBL3375349

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Functional
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia.
Cheng W, Yuan Y, Qiu N, Peng P, Sheng R, Hu Y.
Bioorg Med Chem (2014) 22 : 6796 -6805
PubMed 25468044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.68 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360609 1 6.55
CHEMBL3360608 1 6.23
CHEMBL3360607 1 6.19
CHEMBL3360603 1 6.17
CHEMBL3360612 1 6.03
CHEMBL3360604 1 5.99
CHEMBL3360610 1 5.86
CHEMBL3360618 1 5.84
CHEMBL3360605 1 5.74
CHEMBL3360602 1 5.69
CHEMBL3360613 1 5.64
CHEMBL3360619 1 5.59
CHEMBL3360616 1 5.59
CHEMBL3360617 1 5.55
CHEMBL3360620 1 5.46
CHEMBL3352899 1 5.37
CHEMBL553 ERLOTINIB 4.0 1 5.36
CHEMBL3360614 1 5.30
CHEMBL939 GEFITINIB 4.0 1 5.28
CHEMBL3360606 1 5.26
CHEMBL3360611 1 5.22
CHEMBL50882 TIRAPAZAMINE 3.0 1 5.03
CHEMBL3360615 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360609 IC50 = 280.0 nM 6.55
CHEMBL3360608 IC50 = 590.0 nM 6.23
CHEMBL3360607 IC50 = 650.0 nM 6.19
CHEMBL3360603 IC50 = 670.0 nM 6.17
CHEMBL3360612 IC50 = 940.0 nM 6.03
CHEMBL3360604 IC50 = 1030.0 nM 5.99
CHEMBL3360610 IC50 = 1370.0 nM 5.86
CHEMBL3360618 IC50 = 1430.0 nM 5.84
CHEMBL3360605 IC50 = 1840.0 nM 5.74
CHEMBL3360602 IC50 = 2060.0 nM 5.69
CHEMBL3360613 IC50 = 2270.0 nM 5.64
CHEMBL3360619 IC50 = 2540.0 nM 5.59
CHEMBL3360616 IC50 = 2590.0 nM 5.59
CHEMBL3360617 IC50 = 2820.0 nM 5.55
CHEMBL3360620 IC50 = 3440.0 nM 5.46
CHEMBL3352899 IC50 = 4300.0 nM 5.37
CHEMBL553 ERLOTINIB IC50 = 4370.0 nM 5.36
CHEMBL3360614 IC50 = 5040.0 nM 5.30
CHEMBL939 GEFITINIB IC50 = 5210.0 nM 5.28
CHEMBL3360606 IC50 = 5520.0 nM 5.26
CHEMBL3360611 IC50 = 6040.0 nM 5.22
CHEMBL50882 TIRAPAZAMINE IC50 = 9450.0 nM 5.03
CHEMBL3360615 IC50 > 50000.0 nM -