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Assay Detail

CHEMBL815359

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Binding
Compound was evaluated for its ability to inhibit the binding of [3H]-colchicine to tubulin in competitive binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tubulin alpha chain (CHEMBL3658)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent
Hahn KM, Humphreys W, Helms AM, Hastie SB, Macdonald TL
Bioorg Med Chem Lett (1991) 1 : 471 -476
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.51 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18981 THIOCOLCHICINE 1 6.16
CHEMBL88059 1 6.12
CHEMBL145740 1 5.60
CHEMBL107 COLCHICINE 4.0 1 5.60
CHEMBL79720 1 4.94
CHEMBL357071 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18981 THIOCOLCHICINE Ki = 700.0 nM 6.16
CHEMBL88059 Ki = 750.0 nM 6.12
CHEMBL145740 Ki = 2500.0 nM 5.60
CHEMBL107 COLCHICINE Ki = 2500.0 nM 5.60
CHEMBL79720 Ki = 11500.0 nM 4.94
CHEMBL357071 Ki = 22000.0 nM 4.66