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Assay Detail

CHEMBL4481458

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

Binding
Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Somatostatin receptor type 5 (CHEMBL1792)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an SSTR2-Targeting Maytansinoid Conjugate (PEN-221) with Potent Activity in Vitro and in Vivo.
White BH, Whalen K, Kriksciukaite K, Alargova R, Au Yeung T, Bazinet P, Brockman A, DuPont M, Oller H, Lemelin CA, Lim Soo P, Moreau B, Perino S, Quinn JM, Sharma G, Shinde R, Sweryda-Krawiec B, Wooster R, Bilodeau MT.
J Med Chem (2019) 62 : 2708 -2719
PubMed 30735385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.76 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440072 1 9.49
CHEMBL4527856 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440072 Kd = 0.32 nM 9.49
CHEMBL4527856 Kd = 9.6 nM 8.02