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Assay Detail

CHEMBL1647393

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Functional
Antiproliferative activity against human NCI-N87 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-N87
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-N87 (CHEMBL614197)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Fink BE, Norris D, Mastalerz H, Chen P, Goyal B, Zhao Y, Kim SH, Vite GD, Lee FY, Zhang H, Oppenheimer S, Tokarski JS, Wong TW, Gavai AV.
Bioorg Med Chem Lett (2011) 21 : 781 -785
PubMed 21177105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.52 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248108 1 7.46
CHEMBL1645474 1 7.30
CHEMBL1645473 1 7.22
CHEMBL246284 1 7.08
CHEMBL1645466 1 6.92
CHEMBL1645476 1 6.92
CHEMBL1645467 1 6.85
CHEMBL1645470 1 6.85
CHEMBL1645472 1 6.55
CHEMBL1645462 AC-480 1.0 1 6.35
CHEMBL1645471 1 6.10
CHEMBL1645477 1 5.92
CHEMBL1645469 1 5.48
CHEMBL1645475 1 5.47
CHEMBL1645465 1 5.36
CHEMBL1645463 1 -
CHEMBL1645464 1 -
CHEMBL1645468 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248108 IC50 = 35.0 nM 7.46
CHEMBL1645474 IC50 = 50.0 nM 7.30
CHEMBL1645473 IC50 = 60.0 nM 7.22
CHEMBL246284 IC50 = 83.0 nM 7.08
CHEMBL1645466 IC50 = 120.0 nM 6.92
CHEMBL1645476 IC50 = 120.0 nM 6.92
CHEMBL1645467 IC50 = 140.0 nM 6.85
CHEMBL1645470 IC50 = 140.0 nM 6.85
CHEMBL1645472 IC50 = 280.0 nM 6.55
CHEMBL1645462 AC-480 IC50 = 450.0 nM 6.35
CHEMBL1645471 IC50 = 790.0 nM 6.10
CHEMBL1645477 IC50 = 1210.0 nM 5.92
CHEMBL1645469 IC50 = 3300.0 nM 5.48
CHEMBL1645475 IC50 = 3360.0 nM 5.47
CHEMBL1645465 IC50 = 4400.0 nM 5.36
CHEMBL1645463 IC50 - -
CHEMBL1645464 IC50 - -
CHEMBL1645468 IC50 - -