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Assay Detail

CHEMBL4620770

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

Binding
Inhibition of GST-tagged recombinant human MPS1 expressed in baculovirus expression system using biotin-Ahx-PWDPDDADITEILG as substrate preincubated for 15 mins followed by substrate and 2 mM ATP addition and measured after 60 mins by TR-FRET assay
ChEMBL ↗
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity protein kinase TTK (CHEMBL3983) ↗
Type SINGLE PROTEIN
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 75 7.11 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4632740 — — 1 10.00
CHEMBL4636046 — — 1 9.82
CHEMBL4638914 — — 1 9.70
CHEMBL4645348 — — 1 9.52
CHEMBL4640247 — — 1 9.30
CHEMBL4642491 — — 1 9.30
CHEMBL4642174 — — 1 9.30
CHEMBL4634997 — — 1 9.05
CHEMBL4456085 BAY-1217389 1.0 1 9.00
CHEMBL4646001 — — 1 9.00
CHEMBL4632416 — — 1 8.89
CHEMBL4634949 — — 1 8.89
CHEMBL4469414 LUVIXASERTIB 2.0 1 8.89
CHEMBL4632648 — — 1 8.85
CHEMBL4638962 — — 1 8.85
CHEMBL4645182 — — 1 8.82
CHEMBL4303241 BAY-1161909 2.0 1 8.77
CHEMBL4635693 — — 1 8.70
CHEMBL4638150 — — 1 8.46
CHEMBL4646772 — — 1 8.12
CHEMBL4581793 — — 1 8.00
CHEMBL4641881 — — 1 7.29
CHEMBL4640148 — — 1 7.26
CHEMBL4649817 — — 1 7.21
CHEMBL4635532 — — 1 7.11
CHEMBL4637496 — — 1 7.07
CHEMBL4633081 — — 1 6.98
CHEMBL4632856 — — 1 6.96
CHEMBL4649445 — — 1 6.89
CHEMBL4634241 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4632740 — IC50 = 0.1 nM 10.00
CHEMBL4636046 — IC50 = 0.15 nM 9.82
CHEMBL4638914 — IC50 = 0.2 nM 9.70
CHEMBL4645348 — IC50 = 0.3 nM 9.52
CHEMBL4640247 — IC50 = 0.5 nM 9.30
CHEMBL4642491 — IC50 = 0.5 nM 9.30
CHEMBL4642174 — IC50 = 0.5 nM 9.30
CHEMBL4634997 — IC50 = 0.9 nM 9.05
CHEMBL4456085 BAY-1217389 IC50 = 1.0 nM 9.00
CHEMBL4646001 — IC50 = 1.0 nM 9.00
CHEMBL4632416 — IC50 = 1.3 nM 8.89
CHEMBL4634949 — IC50 = 1.3 nM 8.89
CHEMBL4469414 LUVIXASERTIB IC50 = 1.3 nM 8.89
CHEMBL4638962 — IC50 = 1.4 nM 8.85
CHEMBL4632648 — IC50 = 1.4 nM 8.85
CHEMBL4645182 — IC50 = 1.5 nM 8.82
CHEMBL4303241 BAY-1161909 IC50 = 1.7 nM 8.77
CHEMBL4635693 — IC50 = 2.0 nM 8.70
CHEMBL4638150 — IC50 = 3.5 nM 8.46
CHEMBL4646772 — IC50 = 7.6 nM 8.12
CHEMBL4581793 — IC50 = 10.0 nM 8.00
CHEMBL4641881 — IC50 = 51.0 nM 7.29
CHEMBL4640148 — IC50 = 55.0 nM 7.26
CHEMBL4649817 — IC50 = 61.0 nM 7.21
CHEMBL4635532 — IC50 = 77.0 nM 7.11
CHEMBL4637496 — IC50 = 85.0 nM 7.07
CHEMBL4633081 — IC50 = 105.0 nM 6.98
CHEMBL4632856 — IC50 = 111.0 nM 6.96
CHEMBL4649445 — IC50 = 130.0 nM 6.89
CHEMBL4634241 — IC50 = 130.0 nM 6.89
CHEMBL4644831 — IC50 = 140.0 nM 6.85
CHEMBL4647298 — IC50 = 174.0 nM 6.76
CHEMBL3908648 — IC50 = 200.0 nM 6.70
CHEMBL3410060 — IC50 = 230.0 nM 6.64
CHEMBL4646296 — IC50 = 270.0 nM 6.57
CHEMBL3940165 — IC50 = 292.0 nM 6.54
CHEMBL4643612 — IC50 = 300.0 nM 6.52
CHEMBL4646621 — IC50 = 364.0 nM 6.44
CHEMBL4639541 — IC50 = 383.0 nM 6.42
CHEMBL4649409 — IC50 = 435.0 nM 6.36
CHEMBL4632548 — IC50 = 437.0 nM 6.36
CHEMBL4646380 — IC50 = 483.0 nM 6.32
CHEMBL3410069 — IC50 = 561.0 nM 6.25
CHEMBL4637247 — IC50 = 573.0 nM 6.24
CHEMBL4643900 — IC50 = 667.0 nM 6.18
CHEMBL4632986 — IC50 = 670.0 nM 6.17
CHEMBL4635026 — IC50 = 726.0 nM 6.14
CHEMBL4646785 — IC50 = 825.0 nM 6.08
CHEMBL4643569 — IC50 = 900.0 nM 6.05
CHEMBL4632931 — IC50 = 1020.0 nM 5.99