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Assay Detail

CHEMBL1827218

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

Binding
Binding affinity to Aurora A kinase catalytic domain by competitive binding assay
37
Total Activities
37
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

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G.
Bioorg Med Chem Lett (2011) 21 : 5296 -5300
PubMed 21802948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 37 7.76 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572878 TOZASERTIB 2.0 1 8.40
CHEMBL1822648 1 8.30
CHEMBL1822651 1 8.30
CHEMBL1822649 1 8.22
CHEMBL1822661 1 8.15
CHEMBL1822487 1 8.15
CHEMBL1822490 1 8.15
CHEMBL1822653 1 8.15
CHEMBL1822652 1 8.10
CHEMBL1822650 1 8.10
CHEMBL1822638 1 8.10
CHEMBL1822640 1 8.10
CHEMBL1822655 1 8.05
CHEMBL1822637 1 8.05
CHEMBL1822656 1 8.00
CHEMBL1822489 1 8.00
CHEMBL1822654 1 7.96
CHEMBL1822647 1 7.92
CHEMBL1822485 1 7.92
CHEMBL1822659 1 7.89
CHEMBL1822495 1 7.85
CHEMBL1822658 1 7.82
CHEMBL1822639 1 7.82
CHEMBL1822641 1 7.77
CHEMBL1822657 1 7.77
CHEMBL1822488 1 7.64
CHEMBL1822660 1 7.58
CHEMBL1822494 1 7.51
CHEMBL1822491 1 7.50
CHEMBL1822486 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572878 TOZASERTIB Kd = 4.0 nM 8.40
CHEMBL1822648 Kd = 5.0 nM 8.30
CHEMBL1822651 Kd = 5.0 nM 8.30
CHEMBL1822649 Kd = 6.0 nM 8.22
CHEMBL1822661 Kd = 7.0 nM 8.15
CHEMBL1822487 Kd = 7.0 nM 8.15
CHEMBL1822490 Kd = 7.0 nM 8.15
CHEMBL1822653 Kd = 7.0 nM 8.15
CHEMBL1822652 Kd = 8.0 nM 8.10
CHEMBL1822650 Kd = 8.0 nM 8.10
CHEMBL1822638 Kd = 8.0 nM 8.10
CHEMBL1822640 Kd = 8.0 nM 8.10
CHEMBL1822655 Kd = 9.0 nM 8.05
CHEMBL1822637 Kd = 9.0 nM 8.05
CHEMBL1822489 Kd = 10.0 nM 8.00
CHEMBL1822656 Kd = 10.0 nM 8.00
CHEMBL1822654 Kd = 11.0 nM 7.96
CHEMBL1822485 Kd = 12.0 nM 7.92
CHEMBL1822647 Kd = 12.0 nM 7.92
CHEMBL1822659 Kd = 13.0 nM 7.89
CHEMBL1822495 Kd = 14.0 nM 7.85
CHEMBL1822658 Kd = 15.0 nM 7.82
CHEMBL1822639 Kd = 15.0 nM 7.82
CHEMBL1822641 Kd = 17.0 nM 7.77
CHEMBL1822657 Kd = 17.0 nM 7.77
CHEMBL1822488 Kd = 23.0 nM 7.64
CHEMBL1822660 Kd = 26.0 nM 7.58
CHEMBL1822494 Kd = 31.0 nM 7.51
CHEMBL1822491 Kd = 32.0 nM 7.50
CHEMBL1822486 Kd = 38.0 nM 7.42
CHEMBL1822642 Kd = 53.0 nM 7.28
CHEMBL1822645 Kd = 58.0 nM 7.24
CHEMBL1822493 Kd = 85.0 nM 7.07
CHEMBL1822644 Kd = 111.0 nM 6.96
CHEMBL1822492 Kd = 143.0 nM 6.84
CHEMBL1822643 Kd = 301.0 nM 6.52
CHEMBL1822646 Kd = 381.0 nM 6.42