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Assay Detail

CHEMBL4604963

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

Functional
Induction of cell proliferation in rat beta cells incubated for 4 days by EdU incorporation assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Pancreatic beta cell
Confidence 1 — Organism
Curated By Autocuration

Publication

Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Liu YA, Jin Q, Zou Y, Ding Q, Yan S, Wang Z, Hao X, Nguyen B, Zhang X, Pan J, Mo T, Jacobsen K, Lam T, Wu TY, Petrassi HM, Bursulaya B, DiDonato M, Gordon WP, Liu B, Baaten J, Hill R, Nguyen-Tran V, Qiu M, Zhang YQ, Kamireddy A, Espinola S, Deaton L, Ha S, Harb G, Jia Y, Li J, Shen W, Schumacher AM, Colman K, Glynne R, Pan S, McNamara P, Laffitte B, Meeusen S, Molteni V, Loren J.
J Med Chem (2020) 63 : 2958 -2973
PubMed 32077280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.09 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4647659 1 6.72
CHEMBL4638292 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4647659 EC50 = 190.0 nM 6.72
CHEMBL4638292 EC50 = 3500.0 nM 5.46