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Assay Detail

CHEMBL947137

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

Functional
Survival of human HEK293 cells after 48 hrs by MTS reduction assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 1 — Organism
Curated By Autocuration

Target

HEK293 (CHEMBL614818)
Type CELL-LINE
Organism Homo sapiens

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 5.68 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270687 MERIOLIN 5 1 7.07
CHEMBL406463 MERIOLIN 6 1 7.05
CHEMBL406464 MERIOLIN 4 1 6.66
CHEMBL270686 MERIOLIN 3 1 6.62
CHEMBL270897 MERIOLIN 2 1 6.02
CHEMBL411704 1 5.72
CHEMBL405665 MERIOLIN 1 1 5.66
CHEMBL271597 1 4.97
CHEMBL402443 1 4.45
CHEMBL270926 1 4.18
CHEMBL405200 1 4.08
CHEMBL271195 1 -
CHEMBL270346 MERIOLIN 9 1 -
CHEMBL406102 MERIOLIN 8 1 -
CHEMBL405074 MERIOLIN 7 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270687 MERIOLIN 5 IC50 = 85.0 nM 7.07
CHEMBL406463 MERIOLIN 6 IC50 = 89.0 nM 7.05
CHEMBL406464 MERIOLIN 4 IC50 = 220.0 nM 6.66
CHEMBL270686 MERIOLIN 3 IC50 = 240.0 nM 6.62
CHEMBL270897 MERIOLIN 2 IC50 = 960.0 nM 6.02
CHEMBL411704 IC50 = 1920.0 nM 5.72
CHEMBL405665 MERIOLIN 1 IC50 = 2200.0 nM 5.66
CHEMBL271597 IC50 = 10800.0 nM 4.97
CHEMBL402443 IC50 = 35500.0 nM 4.45
CHEMBL270926 IC50 = 66000.0 nM 4.18
CHEMBL405200 IC50 = 84000.0 nM 4.08
CHEMBL271195 IC50 > 100000.0 nM -
CHEMBL270346 MERIOLIN 9 IC50 > 30000.0 nM -
CHEMBL406102 MERIOLIN 8 IC50 > 30000.0 nM -
CHEMBL405074 MERIOLIN 7 IC50 > 100000.0 nM -