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Assay Detail

CHEMBL3369648

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Functional
Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H441
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H441 (CHEMBL1075542)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer.
Jia H, Dai G, Weng J, Zhang Z, Wang Q, Zhou F, Jiao L, Cui Y, Ren Y, Fan S, Zhou J, Qing W, Gu Y, Wang J, Sai Y, Su W.
J Med Chem (2014) 57 : 7577 -7589
PubMed 25148209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.99 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3334567 SAVOLITINIB 3.0 1 8.22
CHEMBL3334569 1 7.80
CHEMBL3334556 1 7.60
CHEMBL3334557 1 7.18
CHEMBL3334551 1 7.18
CHEMBL3334552 1 7.16
CHEMBL3334542 1 7.14
CHEMBL3334564 1 7.14
CHEMBL3334561 1 7.11
CHEMBL3334540 1 6.98
CHEMBL3334568 1 6.95
CHEMBL3334565 1 6.94
CHEMBL3334570 1 6.78
CHEMBL3334562 1 6.76
CHEMBL3334541 1 6.75
CHEMBL3334560 1 6.75
CHEMBL3334546 1 6.74
CHEMBL3334550 1 6.74
CHEMBL3334563 1 6.69
CHEMBL3334549 1 6.54
CHEMBL3334544 1 6.37
CHEMBL3334545 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3334567 SAVOLITINIB IC50 = 6.0 nM 8.22
CHEMBL3334569 IC50 = 16.0 nM 7.80
CHEMBL3334556 IC50 = 25.0 nM 7.60
CHEMBL3334557 IC50 = 66.0 nM 7.18
CHEMBL3334551 IC50 = 66.0 nM 7.18
CHEMBL3334552 IC50 = 70.0 nM 7.16
CHEMBL3334542 IC50 = 73.0 nM 7.14
CHEMBL3334564 IC50 = 73.0 nM 7.14
CHEMBL3334561 IC50 = 77.0 nM 7.11
CHEMBL3334540 IC50 = 104.0 nM 6.98
CHEMBL3334568 IC50 = 113.0 nM 6.95
CHEMBL3334565 IC50 = 116.0 nM 6.94
CHEMBL3334570 IC50 = 165.0 nM 6.78
CHEMBL3334562 IC50 = 172.0 nM 6.76
CHEMBL3334541 IC50 = 178.0 nM 6.75
CHEMBL3334560 IC50 = 177.0 nM 6.75
CHEMBL3334546 IC50 = 183.0 nM 6.74
CHEMBL3334550 IC50 = 184.0 nM 6.74
CHEMBL3334563 IC50 = 203.0 nM 6.69
CHEMBL3334549 IC50 = 287.0 nM 6.54
CHEMBL3334544 IC50 = 425.0 nM 6.37
CHEMBL3334545 IC50 = 443.0 nM 6.35