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Assay Detail

CHEMBL3888080

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Binding
In Vitro Aurora A Activity Assay (DiscoverX): Reactions were carried out at room temperature in 15 mM HEPES buffer (pH 7.4) containing 20 mM NaCl, 1 mM EGTA, 0.02% Tween 20, 10 mM MgCl2, 5% (v/v) DMSO, and 2.3 nM Aurora A Inhibitor was added to the mixture, and the reaction was initiated by the addition of 75 uM ATP and 2 mM peptide substrate. All kinetic assays were performed in 384-well plates using a Wallac Envision 2102 plate reader (Perkin Elmer).
ChEMBL ↗
80
Total Activities
80
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Aurora kinase inhibitors and methods of making and using thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 7.03 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
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
CHEMBL2170411 — — 1 7.67
CHEMBL2170415 — — 1 7.67
CHEMBL2170412 — — 1 7.63
CHEMBL2170409 — — 1 7.57
CHEMBL2170590 — — 1 7.55

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
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
CHEMBL2170590 — IC50 = 28.1 nM 7.55
CHEMBL3958960 — IC50 = 28.0 nM 7.55
CHEMBL2170442 — IC50 = 30.2 nM 7.52
CHEMBL3971129 — IC50 = 30.2 nM 7.52
CHEMBL2170434 — IC50 = 35.0 nM 7.46
CHEMBL2170439 — IC50 = 35.0 nM 7.46
CHEMBL3962346 — 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
CHEMBL3969926 — 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
CHEMBL3970534 — IC50 = 186.5 nM 6.73
CHEMBL2170591 — 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