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Assay Detail

CHEMBL5320451

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

Binding
Inhibition of Nano-Luc fused PIKFYVE (unknown origin) expressed in HEK293T cells pretreated for 3 hrs followed by K8-tarcer addition and measured after 1 hr by NanoBRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

1-phosphatidylinositol 3-phosphate 5-kinase (CHEMBL1938222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1.
Lu W, Liu Y, Gao Y, Geng Q, Gurbani D, Li L, Ficarro SB, Meyer CJ, Sinha D, You I, Tse J, He Z, Ji W, Che J, Kim AY, Yu T, Wen K, Anderson KC, Marto JA, Westover KD, Zhang T, Gray NS.
J Med Chem (2023) 66 : 3356 -3371
PubMed 36826833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.47 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297643 APILIMOD 2.0 1 8.40
CHEMBL5413843 1 6.54
CHEMBL5398852 1 -
CHEMBL5415114 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297643 APILIMOD IC50 = 4.0 nM 8.40
CHEMBL5413843 IC50 = 292.0 nM 6.54
CHEMBL5398852 IC50 > 3000.0 nM -
CHEMBL5415114 IC50 > 3000.0 nM -