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Assay Detail

CHEMBL860208

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Binding
Inhibition of ERK2
6
Total Activities
6
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

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

Publication

Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM.
J Med Chem (2006) 49 : 3563 -3580
PubMed 16759099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.33 5.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378627 1 5.41
CHEMBL210618 1 5.33
CHEMBL210963 1 5.24
CHEMBL208637 1 -
CHEMBL210928 1 -
CHEMBL210032 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378627 Ki = 3900.0 nM 5.41
CHEMBL210618 Ki = 4700.0 nM 5.33
CHEMBL210963 Ki = 5800.0 nM 5.24
CHEMBL208637 Ki > 8800.0 nM -
CHEMBL210928 Ki > 8800.0 nM -
CHEMBL210032 Ki > 8800.0 nM -