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Assay Detail

CHEMBL5578848

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

Binding
Inhibition of ERK phosphorylation in human KYSE520 cells incubated for 2 hrs by HTRF method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type KYSE520
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of JAB-3312, a Potent SHP2 Allosteric Inhibitor for Cancer Treatment.
Ma C, Kang D, Gao P, Zhang W, Wu X, Xu Z, Han H, Zhang L, Cai Y, Wang Y, Wang Y, Long W.
J Med Chem (2024) 67 : 13534 -13549
PubMed 39110625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.79 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4752051 1 9.60
CHEMBL5591213 1 9.40
CHEMBL4745425 1 9.36
CHEMBL4789817 1 9.01
CHEMBL5591400 1 9.01
CHEMBL4752599 1 8.85
CHEMBL5591410 1 8.62
CHEMBL5595416 1 8.59
CHEMBL4752704 1 7.77
CHEMBL5595838 1 7.64
CHEMBL5583655 1 -
CHEMBL5591249 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4752051 IC50 = 0.25 nM 9.60
CHEMBL5591213 IC50 = 0.4 nM 9.40
CHEMBL4745425 IC50 = 0.44 nM 9.36
CHEMBL4789817 IC50 = 0.98 nM 9.01
CHEMBL5591400 IC50 = 0.98 nM 9.01
CHEMBL4752599 IC50 = 1.4 nM 8.85
CHEMBL5591410 IC50 = 2.4 nM 8.62
CHEMBL5595416 IC50 = 2.6 nM 8.59
CHEMBL4752704 IC50 = 17.0 nM 7.77
CHEMBL5595838 IC50 = 23.0 nM 7.64
CHEMBL5583655 IC50 - -
CHEMBL5591249 IC50 - -