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Assay Detail

CHEMBL2026542

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

Binding
Binding affinity to bovine tubulin after 1 hr by spectrofluorometric analysis
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
Yamazaki Y, Tanaka K, Nicholson B, Deyanat-Yazdi G, Potts B, Yoshida T, Oda A, Kitagawa T, Orikasa S, Kiso Y, Yasui H, Akamatsu M, Chinen T, Usui T, Shinozaki Y, Yakushiji F, Miller BR, Neuteboom S, Palladino M, Kanoh K, Lloyd GK, Hayashi Y.
J Med Chem (2012) 55 : 1056 -1071
PubMed 22185476 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 48 5.63 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2024544 1 6.70
CHEMBL2024561 1 6.21
CHEMBL2024542 1 6.16
CHEMBL1096380 PLINABULIN 3.0 1 6.00
CHEMBL2024100 1 5.96
CHEMBL2022198 1 5.92
CHEMBL2024546 1 5.80
CHEMBL2024550 1 5.72
CHEMBL2024101 1 5.70
CHEMBL2024545 1 5.60
CHEMBL2024537 1 5.58
CHEMBL2024538 1 5.54
CHEMBL107 COLCHICINE 4.0 1 5.48
CHEMBL2022197 1 5.35
CHEMBL2024099 1 5.34
CHEMBL2024098 1 5.31
CHEMBL2024097 1 5.13
CHEMBL2024540 1 5.10
CHEMBL2024539 1 5.05
CHEMBL2024543 1 4.93
CHEMBL2022195 1 -
CHEMBL67 COMBRETASTATIN A4 -1.0 1 -
CHEMBL2022208 1 -
CHEMBL2022207 1 -
CHEMBL2022206 1 -
CHEMBL2022205 1 -
CHEMBL2022204 1 -
CHEMBL2022203 1 -
CHEMBL2022202 1 -
CHEMBL2022201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2024544 Kd = 200.0 nM 6.70
CHEMBL2024561 Kd = 620.0 nM 6.21
CHEMBL2024542 Kd = 700.0 nM 6.16
CHEMBL1096380 PLINABULIN Kd = 1000.0 nM 6.00
CHEMBL2024100 Kd = 1100.0 nM 5.96
CHEMBL2022198 Kd = 1200.0 nM 5.92
CHEMBL2024546 Kd = 1600.0 nM 5.80
CHEMBL2024550 Kd = 1900.0 nM 5.72
CHEMBL2024101 Kd = 2000.0 nM 5.70
CHEMBL2024545 Kd = 2500.0 nM 5.60
CHEMBL2024537 Kd = 2600.0 nM 5.58
CHEMBL2024538 Kd = 2900.0 nM 5.54
CHEMBL107 COLCHICINE Kd = 3300.0 nM 5.48
CHEMBL2022197 Kd = 4500.0 nM 5.35
CHEMBL2024099 Kd = 4600.0 nM 5.34
CHEMBL2024098 Kd = 4900.0 nM 5.31
CHEMBL2024097 Kd = 7400.0 nM 5.13
CHEMBL2024540 Kd = 8000.0 nM 5.10
CHEMBL2024539 Kd = 8900.0 nM 5.05
CHEMBL2024543 Kd = 11800.0 nM 4.93
CHEMBL2024549 Kd - -
CHEMBL2024547 Kd - -
CHEMBL2024551 Kd - -
CHEMBL2024552 Kd - -
CHEMBL2024553 Kd - -
CHEMBL2024554 Kd - -
CHEMBL2024555 Kd - -
CHEMBL2024556 Kd - -
CHEMBL2024557 Kd - -
CHEMBL2024558 Kd - -
CHEMBL2024559 Kd - -
CHEMBL2024560 Kd - -
CHEMBL2022194 Kd - -
CHEMBL2024548 Kd - -
CHEMBL2022196 Kd - -
CHEMBL2024541 Kd - -
CHEMBL2022199 Kd - -
CHEMBL2022200 Kd - -
CHEMBL2022201 Kd - -
CHEMBL2022202 Kd - -
CHEMBL2022203 Kd - -
CHEMBL2022204 Kd - -
CHEMBL2022205 Kd - -
CHEMBL2022206 Kd - -
CHEMBL2022207 Kd - -
CHEMBL2022208 Kd - -
CHEMBL67 COMBRETASTATIN A4 Kd - -
CHEMBL2022195 Kd - -