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Assay Detail

CHEMBL4620796

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Functional
Antiproliferative activity against human HT-29 cells after 96 hrs by crystal violet staining based assay
4
Total Activities
4
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

Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase.
Schulze VK, Klar U, Kosemund D, Wengner AM, Siemeister G, Stöckigt D, Neuhaus R, Lienau P, Bader B, Prechtl S, Holton SJ, Briem H, Marquardt T, Schirok H, Jautelat R, Bohlmann R, Nguyen D, Fernández-Montalván AE, Bömer U, Eberspaecher U, Brüning M, Döhr O, Raschke M, Kreft B, Mumberg D, Ziegelbauer K, Brands M, von Nussbaum F, Koppitz M.
J Med Chem (2020) 63 : 8025 -8042
PubMed 32338514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.69 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456085 BAY-1217389 1.0 1 7.21
CHEMBL4640247 1 6.74
CHEMBL4645348 1 6.56
CHEMBL4469414 LUVIXASERTIB 2.0 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456085 BAY-1217389 IC50 = 62.0 nM 7.21
CHEMBL4640247 IC50 = 183.0 nM 6.74
CHEMBL4645348 IC50 = 276.0 nM 6.56
CHEMBL4469414 LUVIXASERTIB IC50 = 557.0 nM 6.25