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Assay Detail

CHEMBL923203

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Functional
Antiproliferative activity against human HT29 cells
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

5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Mastalerz H, Chang M, Chen P, Fink BE, Gavai A, Han WC, Johnson W, Langley D, Lee FY, Leavitt K, Marathe P, Norris D, Oppenheimer S, Sleczka B, Tarrant J, Tokarski JS, Vite GD, Vyas DM, Wong H, Wong TW, Zhang H, Zhang G.
Bioorg Med Chem Lett (2007) 17 : 4947 -4954
PubMed 17606372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.33 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248116 1 5.70
CHEMBL391387 1 5.57
CHEMBL391778 1 5.54
CHEMBL248115 1 5.46
CHEMBL248321 1 5.46
CHEMBL392273 1 5.44
CHEMBL393848 1 5.41
CHEMBL248108 1 5.37
CHEMBL392664 1 5.30
CHEMBL247104 1 5.27
CHEMBL393264 1 5.21
CHEMBL246687 1 5.19
CHEMBL391779 1 5.14
CHEMBL247309 1 5.12
CHEMBL246284 1 5.06
CHEMBL247513 1 5.02
CHEMBL246898 1 -
CHEMBL247914 1 -
CHEMBL248322 1 -
CHEMBL247512 1 -
CHEMBL248114 1 -
CHEMBL247916 1 -
CHEMBL247915 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248116 IC50 = 2000.0 nM 5.70
CHEMBL391387 IC50 = 2700.0 nM 5.57
CHEMBL391778 IC50 = 2900.0 nM 5.54
CHEMBL248115 IC50 = 3500.0 nM 5.46
CHEMBL248321 IC50 = 3500.0 nM 5.46
CHEMBL392273 IC50 = 3600.0 nM 5.44
CHEMBL393848 IC50 = 3900.0 nM 5.41
CHEMBL248108 IC50 = 4300.0 nM 5.37
CHEMBL392664 IC50 = 5000.0 nM 5.30
CHEMBL247104 IC50 = 5400.0 nM 5.27
CHEMBL393264 IC50 = 6100.0 nM 5.21
CHEMBL246687 IC50 = 6500.0 nM 5.19
CHEMBL391779 IC50 = 7300.0 nM 5.14
CHEMBL247309 IC50 = 7600.0 nM 5.12
CHEMBL246284 IC50 = 8700.0 nM 5.06
CHEMBL247513 IC50 = 9500.0 nM 5.02
CHEMBL246898 IC50 - -
CHEMBL247914 IC50 > 10000.0 nM -
CHEMBL248322 IC50 > 5000.0 nM -
CHEMBL247512 IC50 > 10000.0 nM -
CHEMBL248114 IC50 > 5000.0 nM -
CHEMBL247916 IC50 > 5000.0 nM -
CHEMBL247915 IC50 > 5000.0 nM -