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Assay Detail

CHEMBL4766286

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

Binding
Inhibition of human ERG
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).
Hamdouchi C,Kahl SD,Patel Lewis A,Cardona GR,Zink RW,Chen K,Eessalu TE,Ficorilli JV,Marcelo MC,Otto KA,Wilbur KL,Lineswala JP,Piper JL,Coffey DS,Sweetana SA,Haas JV,Brooks DA,Pratt EJ,Belin RM,Deeg MA,Ma X,Cannady EA,Johnson JT,Yumibe NP,Chen Q,Maiti P,Montrose-Rafizadeh C,Chen Y,Reifel Miller A
J Med Chem (2016) 59 : 10891 -10916
PubMed 27749056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 - -
Ki 1 5.20 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4781604 1 5.20
CHEMBL3915620 LY2881835 1.0 1 -
CHEMBL4787498 1 -
CHEMBL3955132 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4781604 Ki = 6300.0 nM 5.20
CHEMBL3915620 LY2881835 IC50 > 10000.0 nM -
CHEMBL4787498 IC50 > 10000.0 nM -
CHEMBL3955132 IC50 > 10000.0 nM -