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Assay Detail

CHEMBL5388997

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 tubulin colchicine binding site (unknown origin) assessed as dissociation constant
3
Total Activities
3
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

Target

Tubulin (CHEMBL2095182)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

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 3 7.06 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410715 1 8.52
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.85
CHEMBL107 COLCHICINE 4.0 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410715 Kd = 3.0 nM 8.52
CHEMBL67 COMBRETASTATIN A4 Kd = 140.0 nM 6.85
CHEMBL107 COLCHICINE Kd = 1500.0 nM 5.82