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Assay Detail

CHEMBL1827220

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

Binding
Binding affinity to Aurora C kinase catalytic domain by competitive binding assay
ChEMBL ↗
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 C (CHEMBL3935) ↗
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 8.21 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1822495 — — 1 9.00
CHEMBL1822638 — — 1 8.70
CHEMBL1822637 — — 1 8.70
CHEMBL1822487 — — 1 8.52
CHEMBL1822485 — — 1 8.40
CHEMBL1822490 — — 1 8.30
CHEMBL1822494 — — 1 8.30
CHEMBL572878 TOZASERTIB 2.0 1 8.22
CHEMBL1822491 — — 1 8.22
CHEMBL1822486 — — 1 8.00
CHEMBL1822488 — — 1 7.89
CHEMBL1822492 — — 1 7.85
CHEMBL1822493 — — 1 7.77
CHEMBL1822489 — — 1 7.10
CHEMBL1822650 — — 1 -
CHEMBL1822660 — — 1 -
CHEMBL1822652 — — 1 -
CHEMBL1822653 — — 1 -
CHEMBL1822654 — — 1 -
CHEMBL1822655 — — 1 -
CHEMBL1822656 — — 1 -
CHEMBL1822657 — — 1 -
CHEMBL1822658 — — 1 -
CHEMBL1822659 — — 1 -
CHEMBL1822651 — — 1 -
CHEMBL1822641 — — 1 -
CHEMBL1822640 — — 1 -
CHEMBL1822639 — — 1 -
CHEMBL1822642 — — 1 -
CHEMBL1822661 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1822495 — Kd = 1.0 nM 9.00
CHEMBL1822638 — Kd = 2.0 nM 8.70
CHEMBL1822637 — Kd = 2.0 nM 8.70
CHEMBL1822487 — Kd = 3.0 nM 8.52
CHEMBL1822485 — Kd = 4.0 nM 8.40
CHEMBL1822490 — Kd = 5.0 nM 8.30
CHEMBL1822494 — Kd = 5.0 nM 8.30
CHEMBL572878 TOZASERTIB Kd = 6.0 nM 8.22
CHEMBL1822491 — Kd = 6.0 nM 8.22
CHEMBL1822486 — Kd = 10.0 nM 8.00
CHEMBL1822488 — Kd = 13.0 nM 7.89
CHEMBL1822492 — Kd = 14.0 nM 7.85
CHEMBL1822493 — Kd = 17.0 nM 7.77
CHEMBL1822489 — Kd = 80.0 nM 7.10
CHEMBL1822643 — Kd - — -
CHEMBL1822644 — Kd - — -
CHEMBL1822645 — Kd - — -
CHEMBL1822646 — Kd - — -
CHEMBL1822647 — Kd - — -
CHEMBL1822648 — Kd - — -
CHEMBL1822649 — Kd - — -
CHEMBL1822650 — Kd - — -
CHEMBL1822660 — Kd - — -
CHEMBL1822652 — Kd - — -
CHEMBL1822653 — Kd - — -
CHEMBL1822654 — Kd - — -
CHEMBL1822655 — Kd - — -
CHEMBL1822656 — Kd - — -
CHEMBL1822657 — Kd - — -
CHEMBL1822658 — Kd - — -
CHEMBL1822659 — Kd - — -
CHEMBL1822651 — Kd - — -
CHEMBL1822641 — Kd - — -
CHEMBL1822640 — Kd - — -
CHEMBL1822639 — Kd - — -
CHEMBL1822642 — Kd - — -
CHEMBL1822661 — Kd - — -