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Assay Detail

CHEMBL1809665

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Functional
Antiproliferative activity in human A2780 cells after 72 hrs by CellTiter-Glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.
Caldarelli M, Angiolini M, Disingrini T, Donati D, Guanci M, Nuvoloni S, Posteri H, Quartieri F, Silvagni M, Colombo R.
Bioorg Med Chem Lett (2011) 21 : 4507 -4511
PubMed 21723120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.53 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1807301 1 7.14
CHEMBL1807303 1 7.08
CHEMBL1808343 1 7.08
CHEMBL1808341 1 7.00
CHEMBL1808338 1 6.87
CHEMBL1808340 1 6.82
CHEMBL1807306 1 6.61
CHEMBL1808339 1 6.53
CHEMBL1807302 1 6.39
CHEMBL1807300 1 6.38
CHEMBL1807304 1 6.31
CHEMBL559845 1 6.30
CHEMBL1808336 1 6.27
CHEMBL1808342 1 6.11
CHEMBL1236095 1 6.00
CHEMBL1808337 1 5.54
CHEMBL1807305 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1807301 IC50 = 73.0 nM 7.14
CHEMBL1807303 IC50 = 83.0 nM 7.08
CHEMBL1808343 IC50 = 83.0 nM 7.08
CHEMBL1808341 IC50 = 101.0 nM 7.00
CHEMBL1808338 IC50 = 135.0 nM 6.87
CHEMBL1808340 IC50 = 150.0 nM 6.82
CHEMBL1807306 IC50 = 244.0 nM 6.61
CHEMBL1808339 IC50 = 298.0 nM 6.53
CHEMBL1807302 IC50 = 407.0 nM 6.39
CHEMBL1807300 IC50 = 422.0 nM 6.38
CHEMBL1807304 IC50 = 485.0 nM 6.31
CHEMBL559845 IC50 = 500.0 nM 6.30
CHEMBL1808336 IC50 = 541.0 nM 6.27
CHEMBL1808342 IC50 = 771.0 nM 6.11
CHEMBL1236095 IC50 = 1000.0 nM 6.00
CHEMBL1808337 IC50 = 2858.0 nM 5.54
CHEMBL1807305 IC50 < 16.0 nM -