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Assay Detail

CHEMBL2339920

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

Binding
Agonist activity at dog TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Piotrowski DW, Futatsugi K, Warmus JS, Orr ST, Freeman-Cook KD, Londregan AT, Wei L, Jennings SM, Herr M, Coffey SB, Jiao W, Storer G, Hepworth D, Wang J, Lavergne SY, Chin JE, Hadcock JR, Brenner MB, Wolford AC, Janssen AM, Roush NS, Buxton J, Hinchey T, Kalgutkar AS, Sharma R, Flynn DA.
ACS Med Chem Lett (2013) 4 : 63 -68
PubMed 24900564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2331646 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2331646 EC50 = 6.0 nM 8.22