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Assay Detail

CHEMBL4620772

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiproliferative activity against human HeLa cells after 96 hrs by crystal violet staining based assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
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 31 6.42 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634997 1 8.34
CHEMBL4456085 BAY-1217389 1.0 1 8.12
CHEMBL4638914 1 7.58
CHEMBL4645182 1 7.43
CHEMBL4636046 1 7.30
CHEMBL4642491 1 7.24
CHEMBL4632416 1 7.17
CHEMBL4632740 1 7.07
CHEMBL4640261 1 6.92
CHEMBL4636230 1 6.85
CHEMBL4638962 1 6.70
CHEMBL4632648 1 6.61
CHEMBL4635693 1 6.58
CHEMBL4303241 BAY-1161909 2.0 1 6.58
CHEMBL4646001 1 6.57
CHEMBL4581793 1 6.16
CHEMBL4638150 1 6.14
CHEMBL4637496 1 5.89
CHEMBL4635532 1 5.81
CHEMBL4640148 1 5.64
CHEMBL3940165 1 5.61
CHEMBL4632548 1 5.29
CHEMBL4643569 1 5.23
CHEMBL4632856 1 5.16
CHEMBL4641881 1 5.12
CHEMBL4637247 1 5.11
CHEMBL4646621 1 5.02
CHEMBL4633800 1 -
CHEMBL3974070 1 -
CHEMBL4649394 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634997 IC50 = 4.6 nM 8.34
CHEMBL4456085 BAY-1217389 IC50 = 7.6 nM 8.12
CHEMBL4638914 IC50 = 26.0 nM 7.58
CHEMBL4645182 IC50 = 37.0 nM 7.43
CHEMBL4636046 IC50 = 50.0 nM 7.30
CHEMBL4642491 IC50 = 57.0 nM 7.24
CHEMBL4632416 IC50 = 67.0 nM 7.17
CHEMBL4632740 IC50 = 85.0 nM 7.07
CHEMBL4640261 IC50 = 120.0 nM 6.92
CHEMBL4636230 IC50 = 140.0 nM 6.85
CHEMBL4638962 IC50 = 200.0 nM 6.70
CHEMBL4632648 IC50 = 246.0 nM 6.61
CHEMBL4635693 IC50 = 266.0 nM 6.58
CHEMBL4303241 BAY-1161909 IC50 = 260.0 nM 6.58
CHEMBL4646001 IC50 = 270.0 nM 6.57
CHEMBL4581793 IC50 = 695.0 nM 6.16
CHEMBL4638150 IC50 = 725.0 nM 6.14
CHEMBL4637496 IC50 = 1290.0 nM 5.89
CHEMBL4635532 IC50 = 1550.0 nM 5.81
CHEMBL4640148 IC50 = 2300.0 nM 5.64
CHEMBL3940165 IC50 = 2480.0 nM 5.61
CHEMBL4632548 IC50 = 5140.0 nM 5.29
CHEMBL4643569 IC50 = 5900.0 nM 5.23
CHEMBL4632856 IC50 = 7000.0 nM 5.16
CHEMBL4641881 IC50 = 7500.0 nM 5.12
CHEMBL4637247 IC50 = 7730.0 nM 5.11
CHEMBL4646621 IC50 = 9590.0 nM 5.02
CHEMBL4633800 IC50 > 10000.0 nM -
CHEMBL3974070 IC50 > 10000.0 nM -
CHEMBL4649394 IC50 > 3000.0 nM -
CHEMBL4638692 IC50 > 10000.0 nM -