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Assay Detail

CHEMBL2173311

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

Binding
Inhibition of Aurora A kinase expressed in Escherichia coli using LRRASLG as substrate by coupled enzyme assay
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Aurora kinase A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.
Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ.
J Med Chem (2012) 55 : 7392 -7416
PubMed 22803810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 7.44 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170419 1 9.10
CHEMBL2170429 1 8.70
CHEMBL2170435 1 8.68
CHEMBL2170601 1 8.60
CHEMBL2169893 1 8.54
CHEMBL2170418 1 8.52
CHEMBL2170416 1 8.51
CHEMBL2170424 1 8.50
CHEMBL2170436 1 8.48
CHEMBL2170427 1 8.43
CHEMBL2170602 1 8.41
CHEMBL2170431 1 8.40
CHEMBL2170589 1 8.35
CHEMBL2170422 1 8.29
CHEMBL2170592 1 8.21
CHEMBL2170437 1 8.18
CHEMBL2170587 1 8.07
CHEMBL2170597 1 8.00
CHEMBL244793 1 7.95
CHEMBL2170413 1 7.91
CHEMBL2170414 1 7.84
CHEMBL2170417 1 7.76
CHEMBL2170404 1 7.75
CHEMBL2170421 1 7.74
CHEMBL2170441 1 7.73
CHEMBL2170420 1 7.70
CHEMBL2170415 1 7.67
CHEMBL2170411 1 7.67
CHEMBL2170412 1 7.63
CHEMBL2170409 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170419 IC50 = 0.8 nM 9.10
CHEMBL2170429 IC50 = 2.0 nM 8.70
CHEMBL2170435 IC50 = 2.1 nM 8.68
CHEMBL2170601 IC50 = 2.5 nM 8.60
CHEMBL2169893 IC50 = 2.9 nM 8.54
CHEMBL2170418 IC50 = 3.0 nM 8.52
CHEMBL2170416 IC50 = 3.1 nM 8.51
CHEMBL2170424 IC50 = 3.17 nM 8.50
CHEMBL2170436 IC50 = 3.3 nM 8.48
CHEMBL2170427 IC50 = 3.7 nM 8.43
CHEMBL2170602 IC50 = 3.9 nM 8.41
CHEMBL2170431 IC50 = 4.0 nM 8.40
CHEMBL2170589 IC50 = 4.5 nM 8.35
CHEMBL2170422 IC50 = 5.1 nM 8.29
CHEMBL2170592 IC50 = 6.1 nM 8.21
CHEMBL2170437 IC50 = 6.6 nM 8.18
CHEMBL2170587 IC50 = 8.5 nM 8.07
CHEMBL2170597 IC50 = 10.0 nM 8.00
CHEMBL244793 IC50 = 11.3 nM 7.95
CHEMBL2170413 IC50 = 12.3 nM 7.91
CHEMBL2170414 IC50 = 14.4 nM 7.84
CHEMBL2170417 IC50 = 17.3 nM 7.76
CHEMBL2170404 IC50 = 18.0 nM 7.75
CHEMBL2170421 IC50 = 18.3 nM 7.74
CHEMBL2170441 IC50 = 18.7 nM 7.73
CHEMBL2170420 IC50 = 19.9 nM 7.70
CHEMBL2170411 IC50 = 21.4 nM 7.67
CHEMBL2170415 IC50 = 21.2 nM 7.67
CHEMBL2170412 IC50 = 23.2 nM 7.63
CHEMBL2170409 IC50 = 27.0 nM 7.57
CHEMBL2170430 IC50 = 28.0 nM 7.55
CHEMBL2170591 IC50 = 28.1 nM 7.55
CHEMBL2170442 IC50 = 30.2 nM 7.52
CHEMBL2170439 IC50 = 35.0 nM 7.46
CHEMBL2170434 IC50 = 35.1 nM 7.46
CHEMBL2170596 IC50 = 38.2 nM 7.42
CHEMBL2170440 IC50 = 43.0 nM 7.37
CHEMBL2170405 IC50 = 44.9 nM 7.35
CHEMBL2170432 IC50 = 46.6 nM 7.33
CHEMBL2170588 IC50 = 50.2 nM 7.30
CHEMBL394816 IC50 = 57.6 nM 7.24
CHEMBL2170406 IC50 = 71.2 nM 7.15
CHEMBL244839 IC50 = 79.4 nM 7.10
CHEMBL2170408 IC50 = 116.5 nM 6.93
CHEMBL2170586 IC50 = 149.0 nM 6.83
CHEMBL2170590 IC50 = 216.0 nM 6.67
CHEMBL2170410 IC50 = 253.0 nM 6.60
CHEMBL2170598 IC50 = 256.0 nM 6.59
CHEMBL2170438 IC50 = 284.0 nM 6.55
CHEMBL2170599 IC50 = 281.0 nM 6.55