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Assay Detail

CHEMBL968063

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

Binding
Inhibition of SHP2 overexpressed in human KG1 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type KG-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein phosphatase non-receptor type 11 (CHEMBL3864)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adamantyl-substituted retinoid-derived molecules that interact with the orphan nuclear receptor small heterodimer partner: effects of replacing the 1-adamantyl or hydroxyl group on inhibition of cancer cell growth, induction of cancer cell apoptosis, and inhibition of SRC homology 2 domain-containing protein tyrosine phosphatase-2 activity.
Dawson MI, Xia Z, Jiang T, Ye M, Fontana JA, Farhana L, Patel B, Xue LP, Bhuiyan M, Pellicciari R, Macchiarulo A, Nuti R, Zhang XK, Han YH, Tautz L, Hobbs PD, Jong L, Waleh N, Chao WR, Feng GS, Pang Y, Su Y.
J Med Chem (2008) 51 : 5650 -5662
PubMed 18759424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.45 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459711 1 6.35
CHEMBL461827 1 5.74
CHEMBL176252 1 5.68
CHEMBL459497 1 5.68
CHEMBL461415 1 5.64
CHEMBL518627 1 5.41
CHEMBL461620 1 5.34
CHEMBL460351 1 5.27
CHEMBL461199 1 5.19
CHEMBL460350 1 4.99
CHEMBL459712 1 4.70
CHEMBL459710 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459711 IC50 = 450.0 nM 6.35
CHEMBL461827 IC50 = 1830.0 nM 5.74
CHEMBL176252 IC50 = 2100.0 nM 5.68
CHEMBL459497 IC50 = 2110.0 nM 5.68
CHEMBL461415 IC50 = 2270.0 nM 5.64
CHEMBL518627 IC50 = 3910.0 nM 5.41
CHEMBL461620 IC50 = 4550.0 nM 5.34
CHEMBL460351 IC50 = 5370.0 nM 5.27
CHEMBL461199 IC50 = 6400.0 nM 5.19
CHEMBL460350 IC50 = 10200.0 nM 4.99
CHEMBL459712 IC50 = 19900.0 nM 4.70
CHEMBL459710 IC50 = 500000.0 nM -