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Assay Detail

CHEMBL831577

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

Binding
Inhibition of Cyclin B-cyclin-dependent kinase 1
19
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 1/cyclin B (CHEMBL2094127)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.
Lin R, Connolly PJ, Huang S, Wetter SK, Lu Y, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Rugg CA, Middleton SA, Jolliffe LK.
J Med Chem (2005) 48 : 4208 -4211
PubMed 15974571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.95 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261720 2 9.22
CHEMBL361900 1 8.68
CHEMBL363607 2 8.52
CHEMBL425720 1 8.49
CHEMBL187395 1 8.49
CHEMBL364927 1 8.49
CHEMBL370698 1 8.43
CHEMBL190643 1 8.35
CHEMBL363130 1 8.32
CHEMBL191003 JNJ-7706621 2 8.22
CHEMBL189855 1 7.35
CHEMBL190453 1 6.89
CHEMBL190955 1 6.27
CHEMBL189894 1 6.18
CHEMBL190171 1 5.68
CHEMBL187345 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261720 IC50 = 0.6 nM 9.22
CHEMBL261720 IC50 = 0.6 nM 9.22
CHEMBL361900 IC50 = 2.1 nM 8.68
CHEMBL363607 IC50 = 3.0 nM 8.52
CHEMBL187395 IC50 = 3.2 nM 8.49
CHEMBL364927 IC50 = 3.2 nM 8.49
CHEMBL425720 IC50 = 3.2 nM 8.49
CHEMBL370698 IC50 = 3.7 nM 8.43
CHEMBL190643 IC50 = 4.5 nM 8.35
CHEMBL363130 IC50 = 4.8 nM 8.32
CHEMBL191003 JNJ-7706621 IC50 = 6.0 nM 8.22
CHEMBL191003 JNJ-7706621 IC50 = 6.4 nM 8.19
CHEMBL363607 IC50 = 8.0 nM 8.10
CHEMBL189855 IC50 = 45.0 nM 7.35
CHEMBL190453 IC50 = 130.0 nM 6.89
CHEMBL190955 IC50 = 540.0 nM 6.27
CHEMBL189894 IC50 = 660.0 nM 6.18
CHEMBL190171 IC50 = 2100.0 nM 5.68
CHEMBL187345 IC50 > 100000.0 nM -