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Assay Detail

CHEMBL5049203

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

Binding
Inhibition of ERK phosphorylation in human A-375 cells incubated for 3 hrs by DELFIA assay
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-375
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
Poddutoori R, Aardalen K, Aithal K, Barahagar SS, Belliappa C, Bock M, Chelur S, Gerken A, Gopinath S, Gruenenfelder B, Kiffe M, Krishnaswami M, Langowski J, Madapa S, Narayanan K, Pandit C, Panigrahi SK, Perrone M, Potakamuri RK, Ramachandra M, Ramanathan A, Ramos R, Sager E, Samajdar S, Subramanya HS, Thimmasandra DS, Venetsanakos E, Möbitz H.
J Med Chem (2022) 65 : 4350 -4366
PubMed 35195996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.10 6.40
IC50 3 7.08 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3926171 1 7.22
CHEMBL5089865 1 7.10
CHEMBL5080471 1 6.92
CHEMBL5090765 1 6.40
CHEMBL5094993 1 5.52
CHEMBL3904439 1 5.30
CHEMBL5087942 1 5.24
CHEMBL3951042 1 5.16
CHEMBL3974369 1 4.72
CHEMBL3936680 1 4.30
CHEMBL3971755 1 4.19
CHEMBL5085569 1 -
CHEMBL3932078 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3926171 IC50 = 60.0 nM 7.22
CHEMBL5089865 IC50 = 80.0 nM 7.10
CHEMBL5080471 IC50 = 120.0 nM 6.92
CHEMBL5090765 EC50 = 400.0 nM 6.40
CHEMBL5094993 EC50 = 3000.0 nM 5.52
CHEMBL3904439 EC50 = 5000.0 nM 5.30
CHEMBL5087942 EC50 = 5800.0 nM 5.24
CHEMBL3951042 EC50 = 7000.0 nM 5.16
CHEMBL3974369 EC50 = 19000.0 nM 4.72
CHEMBL3936680 EC50 = 50000.0 nM 4.30
CHEMBL3971755 EC50 = 64000.0 nM 4.19
CHEMBL5085569 EC50 = 340000.0 nM -
CHEMBL3932078 EC50 = 109000.0 nM -