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Assay Detail

CHEMBL867341

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Binding
Inhibition of MEK1
ChEMBL ↗
63
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors.
Varaprasad CV, Barawkar D, El Abdellaoui H, Chakravarty S, Allan M, Chen H, Zhang W, Wu JZ, Tam R, Hamatake R, Lang S, Hong Z.
Bioorg Med Chem Lett (2006) 16 : 3975 -3980
PubMed 16725322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 6.39 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375609 — — 1 7.42
CHEMBL213992 — — 1 7.38
CHEMBL213167 — — 1 7.36
CHEMBL211359 — — 1 7.21
CHEMBL377783 — — 1 7.17
CHEMBL211201 — — 1 7.14
CHEMBL213168 — — 1 7.07
CHEMBL213651 — — 1 6.66
CHEMBL385820 — — 1 6.60
CHEMBL377592 — — 1 6.46
CHEMBL425065 — — 1 6.39
CHEMBL380328 — — 1 6.39
CHEMBL213563 — — 1 6.38
CHEMBL212110 — — 1 6.37
CHEMBL378014 — — 1 6.30
CHEMBL378719 — — 1 6.30
CHEMBL212214 — — 1 6.30
CHEMBL209868 — — 1 6.29
CHEMBL209845 — — 1 6.21
CHEMBL212305 — — 1 6.19
CHEMBL378688 — — 1 6.17
CHEMBL209502 — — 1 6.16
CHEMBL212480 — — 2 6.13
CHEMBL378833 — — 1 6.10
CHEMBL212474 — — 1 6.10
CHEMBL377591 — — 1 5.91
CHEMBL209489 — — 1 5.86
CHEMBL209520 — — 1 5.84
CHEMBL213562 — — 1 5.84
CHEMBL375410 — — 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375609 — IC50 = 38.0 nM 7.42
CHEMBL213992 — IC50 = 42.0 nM 7.38
CHEMBL213167 — IC50 = 44.0 nM 7.36
CHEMBL211359 — IC50 = 62.0 nM 7.21
CHEMBL377783 — IC50 = 68.0 nM 7.17
CHEMBL211201 — IC50 = 73.0 nM 7.14
CHEMBL213168 — IC50 = 86.0 nM 7.07
CHEMBL213651 — IC50 = 220.0 nM 6.66
CHEMBL385820 — IC50 = 250.0 nM 6.60
CHEMBL377592 — IC50 = 350.0 nM 6.46
CHEMBL425065 — IC50 = 410.0 nM 6.39
CHEMBL380328 — IC50 = 410.0 nM 6.39
CHEMBL213563 — IC50 = 420.0 nM 6.38
CHEMBL212110 — IC50 = 430.0 nM 6.37
CHEMBL378719 — IC50 = 500.0 nM 6.30
CHEMBL212214 — IC50 = 500.0 nM 6.30
CHEMBL378014 — IC50 = 500.0 nM 6.30
CHEMBL209868 — IC50 = 510.0 nM 6.29
CHEMBL209845 — IC50 = 620.0 nM 6.21
CHEMBL212305 — IC50 = 650.0 nM 6.19
CHEMBL378688 — IC50 = 670.0 nM 6.17
CHEMBL209502 — IC50 = 690.0 nM 6.16
CHEMBL212480 — IC50 = 740.0 nM 6.13
CHEMBL212474 — IC50 = 800.0 nM 6.10
CHEMBL378833 — IC50 = 790.0 nM 6.10
CHEMBL212480 — IC50 = 1200.0 nM 5.92
CHEMBL377591 — IC50 = 1230.0 nM 5.91
CHEMBL209489 — IC50 = 1390.0 nM 5.86
CHEMBL209520 — IC50 = 1450.0 nM 5.84
CHEMBL213562 — IC50 = 1440.0 nM 5.84
CHEMBL375410 — IC50 = 1440.0 nM 5.84
CHEMBL209793 — IC50 = 7000.0 nM 5.16
CHEMBL214349 — IC50 > 5000.0 nM -
CHEMBL208778 — IC50 > 5000.0 nM -
CHEMBL213847 — IC50 > 5000.0 nM -
CHEMBL211546 — IC50 > 5000.0 nM -
CHEMBL377547 — IC50 > 5000.0 nM -
CHEMBL210154 — IC50 > 5000.0 nM -
CHEMBL211382 — IC50 > 5000.0 nM -
CHEMBL211481 — IC50 > 5000.0 nM -
CHEMBL214348 — IC50 > 5000.0 nM -
CHEMBL214067 — IC50 > 5000.0 nM -
CHEMBL378278 — IC50 > 2000.0 nM -
CHEMBL219860 — IC50 > 5000.0 nM -
CHEMBL427239 — IC50 > 5000.0 nM -
CHEMBL378296 — IC50 > 5000.0 nM -
CHEMBL211488 — IC50 > 5000.0 nM -
CHEMBL380295 — IC50 > 5000.0 nM -
CHEMBL378938 — IC50 > 5000.0 nM -
CHEMBL269552 — IC50 > 5000.0 nM -