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Assay Detail

CHEMBL5108375

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

Binding
Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD2 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Publication

Estimating the cooperativity of PROTAC-induced ternary complexes using <sup>19</sup>F NMR displacement assay.
de Castro GV, Ciulli A.
RSC Med Chem (2021) 12 : 1765 -1770
PubMed 34778777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.99 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4226570 1 6.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4226570 Ki = 102.0 nM 6.99