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Assay Detail

CHEMBL3364480

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

Binding
Inhibition of ERK2 in human HepG2 cells assessed as P90RSK phosphorylation at Ser380 after 1.5 hrs by fluorescence assay
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 1 (CHEMBL4040) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.
Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB.
Bioorg Med Chem Lett (2014) 24 : 2635 -2639
PubMed 24813737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.57 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298985 — — 1 8.40
CHEMBL3298199 — — 1 8.15
CHEMBL3298984 — — 1 7.92
CHEMBL3298312 — — 1 7.85
CHEMBL3298982 — — 1 7.77
CHEMBL3298983 — — 1 7.68
CHEMBL3298308 — — 1 7.68
CHEMBL3298418 — — 1 7.64
CHEMBL3298310 — — 1 7.64
CHEMBL3298678 — — 1 7.60
CHEMBL3357950 — — 1 7.46
CHEMBL3357951 — — 1 7.37
CHEMBL3298414 — — 1 7.35
CHEMBL3298309 — — 1 7.29
CHEMBL3297850 — — 1 7.06
CHEMBL3297852 — — 1 6.97
CHEMBL3298311 — — 1 6.96
CHEMBL3297856 — — 1 6.84
CHEMBL3297849 — — 1 6.80
CHEMBL3298417 — — 1 6.70
CHEMBL3297851 — — 1 6.70
CHEMBL3298676 — — 1 6.61
CHEMBL3298307 — — 1 6.48
CHEMBL3298566 — — 1 6.46
CHEMBL3297855 — — 1 6.45
CHEMBL3297853 — — 1 6.43
CHEMBL3298677 — — 1 6.35
CHEMBL3357948 — — 1 6.33
CHEMBL3357949 — — 1 6.29
CHEMBL3298305 — — 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298985 — IC50 = 4.0 nM 8.40
CHEMBL3298199 — IC50 = 7.0 nM 8.15
CHEMBL3298984 — IC50 = 12.0 nM 7.92
CHEMBL3298312 — IC50 = 14.0 nM 7.85
CHEMBL3298982 — IC50 = 17.0 nM 7.77
CHEMBL3298983 — IC50 = 21.0 nM 7.68
CHEMBL3298308 — IC50 = 21.0 nM 7.68
CHEMBL3298418 — IC50 = 23.0 nM 7.64
CHEMBL3298310 — IC50 = 23.0 nM 7.64
CHEMBL3298678 — IC50 = 25.0 nM 7.60
CHEMBL3357950 — IC50 = 35.0 nM 7.46
CHEMBL3357951 — IC50 = 43.0 nM 7.37
CHEMBL3298414 — IC50 = 45.0 nM 7.35
CHEMBL3298309 — IC50 = 51.0 nM 7.29
CHEMBL3297850 — IC50 = 88.0 nM 7.06
CHEMBL3297852 — IC50 = 108.0 nM 6.97
CHEMBL3298311 — IC50 = 110.0 nM 6.96
CHEMBL3297856 — IC50 = 144.0 nM 6.84
CHEMBL3297849 — IC50 = 160.0 nM 6.80
CHEMBL3298417 — IC50 = 198.0 nM 6.70
CHEMBL3297851 — IC50 = 200.0 nM 6.70
CHEMBL3298676 — IC50 = 247.0 nM 6.61
CHEMBL3298307 — IC50 = 330.0 nM 6.48
CHEMBL3298566 — IC50 = 348.0 nM 6.46
CHEMBL3297855 — IC50 = 356.0 nM 6.45
CHEMBL3297853 — IC50 = 368.0 nM 6.43
CHEMBL3298677 — IC50 = 445.0 nM 6.35
CHEMBL3357948 — IC50 = 473.0 nM 6.33
CHEMBL3357949 — IC50 = 513.0 nM 6.29
CHEMBL3298305 — IC50 = 753.0 nM 6.12
CHEMBL3297858 — IC50 = 917.0 nM 6.04
CHEMBL3297848 — IC50 = 1216.0 nM 5.92
CHEMBL3297847 — IC50 = 1628.0 nM 5.79
CHEMBL3298894 — IC50 = 1856.0 nM 5.73
CHEMBL3297854 — IC50 = 2109.0 nM 5.68
CHEMBL3298673 — IC50 = 2138.0 nM 5.67
CHEMBL3298304 — IC50 = 2255.0 nM 5.65
CHEMBL3298306 — IC50 = 2450.0 nM 5.61
CHEMBL3298674 — IC50 = 2611.0 nM 5.58
CHEMBL3297857 — IC50 = 2757.0 nM 5.56
CHEMBL3298416 — IC50 = 3009.0 nM 5.52
CHEMBL3298671 — IC50 = 4384.0 nM 5.36
CHEMBL3298565 — IC50 = 4400.0 nM 5.36
CHEMBL3298672 — IC50 = 6620.0 nM 5.18
CHEMBL3298675 — IC50 = 7438.0 nM 5.13
CHEMBL3298567 — IC50 = 13238.0 nM 4.88