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Assay Detail

CHEMBL4828252

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

Binding
Inhibition of MKN2 (unknown origin) in presence of ATP by HTRF assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Optimization of 4,6-Disubstituted Pyrido[3,2-<i>d</i>]pyrimidines as Dual MNK/PIM Inhibitors to Inhibit Leukemia Cell Growth.
Han Y, Zhang H, Wang S, Li B, Xing K, Shi Y, Cao H, Zhang J, Tong T, Zang J, Guan L, Gao X, Wang Y, Liu D, Huang M, Jing Y, Zhao L.
J Med Chem (2021) 64 : 13719 -13735
PubMed 34515481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.59 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4869634 1 8.15
CHEMBL4872538 1 8.00
CHEMBL4859971 1 7.60
CHEMBL4876307 1 7.58
CHEMBL4857156 1 7.54
CHEMBL4859617 1 7.48
CHEMBL4853562 1 7.44
CHEMBL4861251 1 7.39
CHEMBL4848753 1 7.39
CHEMBL4879010 1 7.37
CHEMBL4858115 1 7.28
CHEMBL4861078 1 7.24
CHEMBL4849911 1 7.21
CHEMBL4864209 1 6.96
CHEMBL4866350 1 6.21
CHEMBL4846164 1 6.21
CHEMBL1240885 1 5.80
CHEMBL4850233 1 5.75
CHEMBL4855483 1 5.72
CHEMBL4866279 1 5.72
CHEMBL4874353 1 5.66
CHEMBL4856576 1 5.60
CHEMBL4872712 1 5.41
CHEMBL4875475 1 5.38
CHEMBL4860143 1 5.32
CHEMBL4848439 1 5.31
CHEMBL4867333 1 5.30
CHEMBL4873909 1 -
CHEMBL4872456 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4869634 IC50 = 7.0 nM 8.15
CHEMBL4872538 IC50 = 10.0 nM 8.00
CHEMBL4859971 IC50 = 25.0 nM 7.60
CHEMBL4876307 IC50 = 26.0 nM 7.58
CHEMBL4857156 IC50 = 29.0 nM 7.54
CHEMBL4859617 IC50 = 33.0 nM 7.48
CHEMBL4853562 IC50 = 36.0 nM 7.44
CHEMBL4861251 IC50 = 41.0 nM 7.39
CHEMBL4848753 IC50 = 41.0 nM 7.39
CHEMBL4879010 IC50 = 43.0 nM 7.37
CHEMBL4858115 IC50 = 52.0 nM 7.28
CHEMBL4861078 IC50 = 58.0 nM 7.24
CHEMBL4849911 IC50 = 62.0 nM 7.21
CHEMBL4864209 IC50 = 111.0 nM 6.96
CHEMBL4866350 IC50 = 612.0 nM 6.21
CHEMBL4846164 IC50 = 624.0 nM 6.21
CHEMBL1240885 IC50 = 1600.0 nM 5.80
CHEMBL4850233 IC50 = 1800.0 nM 5.75
CHEMBL4855483 IC50 = 1900.0 nM 5.72
CHEMBL4866279 IC50 = 1900.0 nM 5.72
CHEMBL4874353 IC50 = 2200.0 nM 5.66
CHEMBL4856576 IC50 = 2500.0 nM 5.60
CHEMBL4872712 IC50 = 3900.0 nM 5.41
CHEMBL4875475 IC50 = 4200.0 nM 5.38
CHEMBL4860143 IC50 = 4800.0 nM 5.32
CHEMBL4848439 IC50 = 4900.0 nM 5.31
CHEMBL4867333 IC50 = 5000.0 nM 5.30
CHEMBL4873909 IC50 > 10000.0 nM -
CHEMBL4872456 IC50 > 10000.0 nM -