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Assay Detail

CHEMBL4406786

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

Binding
Inhibition of human ALK2 R206H mutant using casein as substrate in presence of 10 uM [gamma33P] ATP by radioactive assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Activin receptor type-1 (CHEMBL5903)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ensan D, Smil D, Zepeda-Velázquez CA, Panagopoulos D, Wong JF, Williams EP, Adamson R, Bullock AN, Kiyota T, Aman A, Roberts OG, Edwards AM, O'Meara JA, Isaac MB, Al-Awar R.
J Med Chem (2020) 63 : 4978 -4996
PubMed 32369358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.92 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4435320 1 8.40
CHEMBL4434694 1 8.30
CHEMBL4548795 1 8.22
CHEMBL4440168 1 8.10
CHEMBL4553210 1 8.05
CHEMBL4575655 1 7.72
CHEMBL4575999 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4435320 IC50 = 4.0 nM 8.40
CHEMBL4434694 IC50 = 5.0 nM 8.30
CHEMBL4548795 IC50 = 6.0 nM 8.22
CHEMBL4440168 IC50 = 8.0 nM 8.10
CHEMBL4553210 IC50 = 9.0 nM 8.05
CHEMBL4575655 IC50 = 19.0 nM 7.72
CHEMBL4575999 IC50 = 226.0 nM 6.65