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Assay Detail

CHEMBL3624922

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Binding
Inhibition of MAP4K4 (unknown origin) by Z'LYTE assay
12
Total Activities
12
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

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.
Ndubaku CO, Crawford TD, Chen H, Boggs JW, Drobnick J, Harris SF, Jesudason R, McNamara E, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Vitorino P, Wang L, Wu P, Yeung S, Chen J, Chen K, Ding CZ, Wang T, Xu Z, Gould SE, Murray LJ, Ye W.
ACS Med Chem Lett (2015) 6 : 913 -918
PubMed 26288693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.87 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623135 1 8.85
CHEMBL3623139 1 8.80
CHEMBL3623137 1 8.46
CHEMBL3623136 1 8.43
CHEMBL3623138 1 8.43
CHEMBL3623134 1 7.82
CHEMBL3623128 1 7.75
CHEMBL3623133 1 7.50
CHEMBL3623131 1 7.39
CHEMBL3623129 1 7.34
CHEMBL3262580 1 7.24
CHEMBL3623132 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623135 IC50 = 1.4 nM 8.85
CHEMBL3623139 IC50 = 1.6 nM 8.80
CHEMBL3623137 IC50 = 3.5 nM 8.46
CHEMBL3623136 IC50 = 3.7 nM 8.43
CHEMBL3623138 IC50 = 3.7 nM 8.43
CHEMBL3623134 IC50 = 15.0 nM 7.82
CHEMBL3623128 IC50 = 18.0 nM 7.75
CHEMBL3623133 IC50 = 32.0 nM 7.50
CHEMBL3623131 IC50 = 41.0 nM 7.39
CHEMBL3623129 IC50 = 46.0 nM 7.34
CHEMBL3262580 IC50 = 58.0 nM 7.24
CHEMBL3623132 IC50 = 401.0 nM 6.40