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Assay Detail

CHEMBL3265752

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

Binding
Inhibition of human MAP4K4 using 5-FAM-LGRDKYKTLRQIRQ-COOH as substrate by Z'-LYTE assay
19
Total Activities
19
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

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.
Crawford TD, Ndubaku CO, Chen H, Boggs JW, Bravo BJ, Delatorre K, Giannetti AM, Gould SE, Harris SF, Magnuson SR, McNamara E, Murray LJ, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Stanley M, Vitorino P, Wang L, West K, Wu P, Ye W.
J Med Chem (2014) 57 : 3484 -3493
PubMed 24673130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.54 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3262587 1 7.77
CHEMBL3262580 1 7.24
CHEMBL3262579 1 7.22
CHEMBL3262583 1 7.11
CHEMBL3262570 1 6.92
CHEMBL3262584 1 6.88
CHEMBL3262569 1 6.72
CHEMBL3262575 1 6.65
CHEMBL3262581 1 6.53
CHEMBL3262572 1 6.48
CHEMBL3262578 1 6.46
CHEMBL3262582 1 6.42
CHEMBL3262577 1 6.41
CHEMBL3262574 1 6.37
CHEMBL3262571 1 6.26
CHEMBL3262573 1 6.16
CHEMBL3262576 1 5.77
CHEMBL3262586 1 5.67
CHEMBL3262585 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3262587 IC50 = 17.0 nM 7.77
CHEMBL3262580 IC50 = 58.0 nM 7.24
CHEMBL3262579 IC50 = 60.0 nM 7.22
CHEMBL3262583 IC50 = 77.0 nM 7.11
CHEMBL3262570 IC50 = 121.0 nM 6.92
CHEMBL3262584 IC50 = 132.0 nM 6.88
CHEMBL3262569 IC50 = 189.0 nM 6.72
CHEMBL3262575 IC50 = 225.0 nM 6.65
CHEMBL3262581 IC50 = 297.0 nM 6.53
CHEMBL3262572 IC50 = 330.0 nM 6.48
CHEMBL3262578 IC50 = 351.0 nM 6.46
CHEMBL3262582 IC50 = 381.0 nM 6.42
CHEMBL3262577 IC50 = 387.0 nM 6.41
CHEMBL3262574 IC50 = 423.0 nM 6.37
CHEMBL3262571 IC50 = 546.0 nM 6.26
CHEMBL3262573 IC50 = 689.0 nM 6.16
CHEMBL3262576 IC50 = 1700.0 nM 5.77
CHEMBL3262586 IC50 = 2120.0 nM 5.67
CHEMBL3262585 IC50 = 5840.0 nM 5.23