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Assay Detail

CHEMBL888278

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

Binding
Inhibition of Aurora2
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Lin R, Connolly PJ, Lu Y, Chiu G, Li S, Yu Y, Huang S, Li X, Emanuel SL, Middleton SA, Gruninger RH, Adams M, Fuentes-Pesquera AR, Greenberger LM.
Bioorg Med Chem Lett (2007) 17 : 4297 -4302
PubMed 17532631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.79 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL249500 1 7.39
CHEMBL400569 1 6.55
CHEMBL248891 1 6.50
CHEMBL429478 1 6.44
CHEMBL400906 1 6.00
CHEMBL249303 1 6.00
CHEMBL249304 1 6.00
CHEMBL401064 1 5.44
CHEMBL249518 1 5.43
CHEMBL400568 1 5.40
CHEMBL249519 1 5.10
CHEMBL249302 1 5.00
CHEMBL399042 1 4.00
CHEMBL248713 1 -
CHEMBL248712 1 -
CHEMBL400749 1 -
CHEMBL251740 1 -
CHEMBL251739 1 -
CHEMBL249502 1 -
CHEMBL249501 1 -
CHEMBL400858 1 -
CHEMBL391437 1 -
CHEMBL248890 1 -
CHEMBL249094 1 -
CHEMBL249095 1 -
CHEMBL249096 1 -
CHEMBL400859 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL249500 IC50 = 41.0 nM 7.39
CHEMBL400569 IC50 = 280.0 nM 6.55
CHEMBL248891 IC50 = 320.0 nM 6.50
CHEMBL429478 IC50 = 360.0 nM 6.44
CHEMBL400906 IC50 = 1000.0 nM 6.00
CHEMBL249303 IC50 = 1000.0 nM 6.00
CHEMBL249304 IC50 = 1000.0 nM 6.00
CHEMBL401064 IC50 = 3620.0 nM 5.44
CHEMBL249518 IC50 = 3750.0 nM 5.43
CHEMBL400568 IC50 = 3990.0 nM 5.40
CHEMBL249519 IC50 = 8020.0 nM 5.10
CHEMBL249302 IC50 = 10000.0 nM 5.00
CHEMBL399042 IC50 = 100000.0 nM 4.00
CHEMBL248713 IC50 > 800.0 nM -
CHEMBL248712 IC50 > 1000.0 nM -
CHEMBL400749 IC50 > 1000.0 nM -
CHEMBL251740 IC50 > 100000.0 nM -
CHEMBL251739 IC50 > 10000.0 nM -
CHEMBL249502 IC50 > 100.0 nM -
CHEMBL249501 IC50 > 10000.0 nM -
CHEMBL400858 IC50 - -
CHEMBL391437 IC50 - -
CHEMBL248890 IC50 > 10000.0 nM -
CHEMBL249094 IC50 > 1000.0 nM -
CHEMBL249095 IC50 > 100000.0 nM -
CHEMBL249096 IC50 > 1000.0 nM -
CHEMBL400859 IC50 > 1000.0 nM -