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Assay Detail

CHEMBL5038009

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

Binding
Inhibition of B0AT1 (unknown origin) by FLIPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of novel, potent and orally efficacious inhibitor of neutral amino acid transporter B<sup>0</sup>AT1 (SLC6A19).
Desai J, Patel B, Darji B, Gite A, Panchal N, Bhosale G, Shedage S, Patel S, Kadam P, Patel G, Kumar Srivastava B, Joharapurkar A, Kshirsagar S, Giri P, Bhayani H, Patel A, Ghoshdastidar K, Bandyopadhyay D, Kumar S, Jain M, Sharma R.
Bioorg Med Chem Lett (2021) 53 : 128421 -128421
PubMed 34718128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.08 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93233 CINROMIDE 2.0 1 6.55
CHEMBL5081254 1 5.72
CHEMBL5088149 1 4.70
CHEMBL116590 1 4.36
CHEMBL5085749 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93233 CINROMIDE IC50 = 280.0 nM 6.55
CHEMBL5081254 IC50 = 1900.0 nM 5.72
CHEMBL5088149 IC50 = 20000.0 nM 4.70
CHEMBL116590 IC50 = 44000.0 nM 4.36
CHEMBL5085749 IC50 = 90000.0 nM 4.05