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Assay Detail

CHEMBL711119

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

Binding
Non-competitive inhibition of the dual specificity kinase MEK
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Duncia JV, Santella JB, Higley CA, Pitts WJ, Wityak J, Frietze WE, Rankin FW, Sun JH, Earl RA, Tabaka AC, Teleha CA, Blom KF, Favata MF, Manos EJ, Daulerio AJ, Stradley DA, Horiuchi K, Copeland RA, Scherle PA, Trzaskos JM, Magolda RL, Trainor GL, Wexler RR, Hobbs FW, Olson RE.
Bioorg Med Chem Lett (1998) 8 : 2839 -2844
PubMed 9873633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.86 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329492 1 6.52
CHEMBL95069 1 6.52
CHEMBL94971 1 6.40
CHEMBL317720 1 6.30
CHEMBL100473 U-0126 1 6.30
CHEMBL316510 1 6.16
CHEMBL97406 1 6.05
CHEMBL329698 1 6.05
CHEMBL330393 1 6.05
CHEMBL318939 1 5.96
CHEMBL97724 1 5.85
CHEMBL94565 1 5.72
CHEMBL316635 1 5.72
CHEMBL95400 1 5.70
CHEMBL95728 1 5.68
CHEMBL330195 1 5.68
CHEMBL95057 1 5.68
CHEMBL97067 1 5.55
CHEMBL95905 1 5.50
CHEMBL97586 1 5.35
CHEMBL97205 1 5.32
CHEMBL316536 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329492 IC50 = 300.0 nM 6.52
CHEMBL95069 IC50 = 300.0 nM 6.52
CHEMBL94971 IC50 = 400.0 nM 6.40
CHEMBL317720 IC50 = 500.0 nM 6.30
CHEMBL100473 U-0126 IC50 = 500.0 nM 6.30
CHEMBL316510 IC50 = 700.0 nM 6.16
CHEMBL97406 IC50 = 900.0 nM 6.05
CHEMBL329698 IC50 = 900.0 nM 6.05
CHEMBL330393 IC50 = 900.0 nM 6.05
CHEMBL318939 IC50 = 1100.0 nM 5.96
CHEMBL97724 IC50 = 1400.0 nM 5.85
CHEMBL94565 IC50 = 1900.0 nM 5.72
CHEMBL316635 IC50 = 1900.0 nM 5.72
CHEMBL95400 IC50 = 2000.0 nM 5.70
CHEMBL95728 IC50 = 2100.0 nM 5.68
CHEMBL330195 IC50 = 2100.0 nM 5.68
CHEMBL95057 IC50 = 2100.0 nM 5.68
CHEMBL97067 IC50 = 2800.0 nM 5.55
CHEMBL95905 IC50 = 3200.0 nM 5.50
CHEMBL97586 IC50 = 4500.0 nM 5.35
CHEMBL97205 IC50 = 4800.0 nM 5.32
CHEMBL316536 IC50 = 13500.0 nM 4.87