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Assay Detail

CHEMBL5388995

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

Binding
Displacement of fluorescent probe (R)-(+)-ethyl 5-amino2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamate from calf brain tubulin colchicine binding site assessed as dissociation constant at 0.05 to 70 uM incubated for 30 mins by fluorescence based assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tubulin (CHEMBL2094134)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
Lucena-Agell D, Guillén MJ, Matesanz R, Álvarez-Bernad B, Hortigüela R, Avilés P, Martínez-Díez M, Santamaría-Núñez G, Contreras J, Plaza-Menacho I, Giménez-Abián JF, Oliva MA, Cuevas C, Díaz JF.
J Med Chem (2024) 67 : 2619 -2630
PubMed 38294341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 6.86 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5437532 1 7.70
CHEMBL5418923 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5437532 Kd = 20.0 nM 7.70
CHEMBL5418923 Kd = 960.0 nM 6.02