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Assay Detail

CHEMBL2167306

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

Binding
Binding affinity to Aurora kinase B catalytic domain by competition binding assay
28
Total Activities
28
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 B (CHEMBL2185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.
Liu G, Abraham S, Tran L, Vickers TD, Xu S, Hadd MJ, Quiambao S, Holladay MW, Hua H, Ford Pulido JM, Gunawardane RN, Davis MI, Eichelberger SR, Apuy JL, Gitnick D, Gardner MF, James J, Breider MA, Belli B, Armstrong RC, Treiber DK.
J Med Chem (2012) 55 : 3250 -3260
PubMed 22380736 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 8.43 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163404 1 8.77
CHEMBL2163407 1 8.77
CHEMBL2163394 1 8.72
CHEMBL2163402 1 8.72
CHEMBL2163388 1 8.66
CHEMBL2163398 1 8.62
CHEMBL2163403 1 8.60
CHEMBL2163390 1 8.59
CHEMBL2163410 1 8.54
CHEMBL2163392 1 8.54
CHEMBL2163389 1 8.54
CHEMBL2163387 1 8.51
CHEMBL2163408 1 8.51
CHEMBL2163400 1 8.51
CHEMBL2163396 1 8.49
CHEMBL2163395 1 8.48
CHEMBL2163412 1 8.44
CHEMBL2163391 1 8.43
CHEMBL2163411 1 8.43
CHEMBL2163401 1 8.37
CHEMBL2163413 1 8.24
CHEMBL2163397 1 8.21
CHEMBL2163409 1 8.18
CHEMBL2163406 1 8.18
CHEMBL2163393 1 8.16
CHEMBL1822658 1 8.10
CHEMBL2163399 1 7.85
CHEMBL2163405 1 7.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163404 Kd = 1.7 nM 8.77
CHEMBL2163407 Kd = 1.7 nM 8.77
CHEMBL2163394 Kd = 1.9 nM 8.72
CHEMBL2163402 Kd = 1.9 nM 8.72
CHEMBL2163388 Kd = 2.2 nM 8.66
CHEMBL2163398 Kd = 2.4 nM 8.62
CHEMBL2163403 Kd = 2.5 nM 8.60
CHEMBL2163390 Kd = 2.6 nM 8.59
CHEMBL2163410 Kd = 2.9 nM 8.54
CHEMBL2163392 Kd = 2.9 nM 8.54
CHEMBL2163389 Kd = 2.9 nM 8.54
CHEMBL2163387 Kd = 3.1 nM 8.51
CHEMBL2163408 Kd = 3.1 nM 8.51
CHEMBL2163400 Kd = 3.1 nM 8.51
CHEMBL2163396 Kd = 3.2 nM 8.49
CHEMBL2163395 Kd = 3.3 nM 8.48
CHEMBL2163412 Kd = 3.6 nM 8.44
CHEMBL2163391 Kd = 3.7 nM 8.43
CHEMBL2163411 Kd = 3.7 nM 8.43
CHEMBL2163401 Kd = 4.3 nM 8.37
CHEMBL2163413 Kd = 5.7 nM 8.24
CHEMBL2163397 Kd = 6.1 nM 8.21
CHEMBL2163409 Kd = 6.6 nM 8.18
CHEMBL2163406 Kd = 6.6 nM 8.18
CHEMBL2163393 Kd = 6.9 nM 8.16
CHEMBL1822658 Kd = 8.0 nM 8.10
CHEMBL2163399 Kd = 14.2 nM 7.85
CHEMBL2163405 Kd = 14.8 nM 7.83