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Assay Detail

CHEMBL953116

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

Binding
Inhibition of Plk1
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase PLK1 (CHEMBL3024)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, Bui M, Purkey HE, Evanchik MJ, Yang W.
Bioorg Med Chem Lett (2008) 18 : 5648 -5652
PubMed 18793847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.34 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484473 1 7.68
CHEMBL525911 1 7.50
CHEMBL496337 1 7.38
CHEMBL498190 1 7.32
CHEMBL507529 1 7.30
CHEMBL498191 1 7.23
CHEMBL478028 1 6.92
CHEMBL519858 1 6.83
CHEMBL497167 1 6.68
CHEMBL485295 1 6.65
CHEMBL485497 1 6.56
CHEMBL508139 1 6.38
CHEMBL522392 1 6.33
CHEMBL497158 1 6.32
CHEMBL485496 1 6.19
CHEMBL523233 1 6.15
CHEMBL492055 1 6.01
CHEMBL525907 1 5.89
CHEMBL491850 1 5.83
CHEMBL498189 1 5.49
CHEMBL496125 1 5.34
CHEMBL523423 1 5.34
CHEMBL495926 1 5.23
CHEMBL496954 1 5.11
CHEMBL497159 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484473 IC50 = 21.0 nM 7.68
CHEMBL525911 IC50 = 32.0 nM 7.50
CHEMBL496337 IC50 = 42.0 nM 7.38
CHEMBL498190 IC50 = 48.0 nM 7.32
CHEMBL507529 IC50 = 50.0 nM 7.30
CHEMBL498191 IC50 = 59.0 nM 7.23
CHEMBL478028 IC50 = 121.0 nM 6.92
CHEMBL519858 IC50 = 149.0 nM 6.83
CHEMBL497167 IC50 = 207.0 nM 6.68
CHEMBL485295 IC50 = 225.0 nM 6.65
CHEMBL485497 IC50 = 274.0 nM 6.56
CHEMBL508139 IC50 = 412.0 nM 6.38
CHEMBL522392 IC50 = 464.0 nM 6.33
CHEMBL497158 IC50 = 474.0 nM 6.32
CHEMBL485496 IC50 = 641.0 nM 6.19
CHEMBL523233 IC50 = 703.0 nM 6.15
CHEMBL492055 IC50 = 977.0 nM 6.01
CHEMBL525907 IC50 = 1301.0 nM 5.89
CHEMBL491850 IC50 = 1476.0 nM 5.83
CHEMBL498189 IC50 = 3241.0 nM 5.49
CHEMBL496125 IC50 = 4516.0 nM 5.34
CHEMBL523423 IC50 = 4528.0 nM 5.34
CHEMBL495926 IC50 = 5928.0 nM 5.23
CHEMBL496954 IC50 = 7685.0 nM 5.11
CHEMBL497159 IC50 = 14451.0 nM 4.84