Assay Detail

CHEMBL4604956

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Functional

Induction of cell proliferation in rat beta cells

ChEMBL ↗

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Target

Pancreatic beta cell (CHEMBL614780) ↗

Open DB target context

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Pancreatic beta cell (CHEMBL614780) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Pancreatic beta cell

CHEMBL614780

Anchored from Assay target.

Protein identity Pancreatic beta cell

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Pancreatic beta cell (CHEMBL614780) ↗

Type

CELL-LINE

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	5.74	6.34

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL99203	IODOTUBERCIDIN	—	1	6.34
CHEMBL269538	HARMINE	1.0	1	5.13

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL99203	IODOTUBERCIDIN	EC50	=	460.0	nM	6.34
CHEMBL269538	HARMINE	EC50	=	7480.0	nM	5.13