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Assay Detail

CHEMBL4423398

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Binding
Inhibition of ERK2 (unknown origin) using lipid as substrate after 40 mins by ADP-Glo luminescence assay
34
Total Activities
34
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

Target

Mitogen-activated protein kinase 1 (CHEMBL4040)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent, orally bioavailable ERK1/2 inhibitors with isoindolin-1-one structure by structure-based drug design.
Ji D, Zhang L, Zhu Q, Bai Y, Wu Y, Xu Y.
Eur J Med Chem (2019) 164 : 334 -341
PubMed 30605831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 8.08 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4434915 1 9.15
CHEMBL4571588 1 9.15
CHEMBL4449385 1 9.10
CHEMBL4435679 1 8.96
CHEMBL4532652 1 8.92
CHEMBL4588783 1 8.80
CHEMBL4567212 1 8.72
CHEMBL4458400 1 8.57
CHEMBL4535176 1 8.54
CHEMBL4442577 1 8.51
CHEMBL4533640 1 8.46
CHEMBL4476178 1 8.44
CHEMBL4524371 1 8.27
CHEMBL4547563 1 8.25
CHEMBL4470800 1 8.14
CHEMBL4463859 1 7.95
CHEMBL4569409 1 7.75
CHEMBL4518783 1 7.75
CHEMBL4472237 1 7.70
CHEMBL4473588 1 7.65
CHEMBL4462277 1 7.59
CHEMBL4435286 1 7.52
CHEMBL4554747 1 7.45
CHEMBL4439967 1 7.44
CHEMBL4457070 1 7.42
CHEMBL4471771 1 7.03
CHEMBL4470651 1 6.70
CHEMBL4517851 1 6.20
CHEMBL4529178 1 -
CHEMBL4466965 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4434915 IC50 = 0.7 nM 9.15
CHEMBL4571588 IC50 = 0.7 nM 9.15
CHEMBL4449385 IC50 = 0.8 nM 9.10
CHEMBL4435679 IC50 = 1.1 nM 8.96
CHEMBL4532652 IC50 = 1.2 nM 8.92
CHEMBL4588783 IC50 = 1.6 nM 8.80
CHEMBL4567212 IC50 = 1.9 nM 8.72
CHEMBL4458400 IC50 = 2.7 nM 8.57
CHEMBL4535176 IC50 = 2.9 nM 8.54
CHEMBL4442577 IC50 = 3.1 nM 8.51
CHEMBL4533640 IC50 = 3.5 nM 8.46
CHEMBL4476178 IC50 = 3.6 nM 8.44
CHEMBL4524371 IC50 = 5.4 nM 8.27
CHEMBL4547563 IC50 = 5.6 nM 8.25
CHEMBL4470800 IC50 = 7.2 nM 8.14
CHEMBL4463859 IC50 = 11.2 nM 7.95
CHEMBL4518783 IC50 = 17.6 nM 7.75
CHEMBL4569409 IC50 = 17.8 nM 7.75
CHEMBL4472237 IC50 = 19.8 nM 7.70
CHEMBL4473588 IC50 = 22.3 nM 7.65
CHEMBL4462277 IC50 = 25.6 nM 7.59
CHEMBL4435286 IC50 = 30.4 nM 7.52
CHEMBL4554747 IC50 = 35.6 nM 7.45
CHEMBL4439967 IC50 = 36.3 nM 7.44
CHEMBL4457070 IC50 = 38.4 nM 7.42
CHEMBL4471771 IC50 = 93.3 nM 7.03
CHEMBL4470651 IC50 = 201.0 nM 6.70
CHEMBL4517851 IC50 = 633.0 nM 6.20
CHEMBL4529178 IC50 > 1000.0 nM -
CHEMBL4466965 IC50 > 1000.0 nM -
CHEMBL4457113 IC50 > 1000.0 nM -
CHEMBL4585624 IC50 > 1000.0 nM -
CHEMBL4528740 IC50 > 1000.0 nM -
CHEMBL4446483 IC50 > 1000.0 nM -