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Assay Detail

CHEMBL947130

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Binding
Inhibition of starfish oocyte CDK1/cyclin B
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Marthasterias glacialis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.
Echalier A, Bettayeb K, Ferandin Y, Lozach O, Clément M, Valette A, Liger F, Marquet B, Morris JC, Endicott JA, Joseph B, Meijer L.
J Med Chem (2008) 51 : 737 -751
PubMed 18232649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.44 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270687 MERIOLIN 5 1 8.15
CHEMBL406463 MERIOLIN 6 1 8.10
CHEMBL406464 MERIOLIN 4 1 8.00
CHEMBL270897 MERIOLIN 2 1 7.24
CHEMBL411704 1 7.22
CHEMBL270686 MERIOLIN 3 1 6.77
CHEMBL271597 1 6.62
CHEMBL405665 MERIOLIN 1 1 6.11
CHEMBL405200 1 6.05
CHEMBL406102 MERIOLIN 8 1 5.92
CHEMBL402443 1 5.89
CHEMBL270926 1 5.75
CHEMBL271195 1 5.66
CHEMBL270346 MERIOLIN 9 1 4.60
CHEMBL405074 MERIOLIN 7 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270687 MERIOLIN 5 IC50 = 7.0 nM 8.15
CHEMBL406463 MERIOLIN 6 IC50 = 8.0 nM 8.10
CHEMBL406464 MERIOLIN 4 IC50 = 10.0 nM 8.00
CHEMBL270897 MERIOLIN 2 IC50 = 57.0 nM 7.24
CHEMBL411704 IC50 = 60.0 nM 7.22
CHEMBL270686 MERIOLIN 3 IC50 = 170.0 nM 6.77
CHEMBL271597 IC50 = 240.0 nM 6.62
CHEMBL405665 MERIOLIN 1 IC50 = 780.0 nM 6.11
CHEMBL405200 IC50 = 900.0 nM 6.05
CHEMBL406102 MERIOLIN 8 IC50 = 1200.0 nM 5.92
CHEMBL402443 IC50 = 1300.0 nM 5.89
CHEMBL270926 IC50 = 1800.0 nM 5.75
CHEMBL271195 IC50 = 2200.0 nM 5.66
CHEMBL270346 MERIOLIN 9 IC50 = 25000.0 nM 4.60
CHEMBL405074 MERIOLIN 7 IC50 = 35000.0 nM 4.46