Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4714985

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

Binding
Inhibition of ACVR2A (unknown origin) using biotin- labelled KTLQDLVYDLSTSGSGSGLPLFVQRTVART substrate in presence of [gamma33P] ATP measured after 20 min
29
Total Activities
29
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-2A (CHEMBL5616)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Selective Transforming Growth Factor β Type II Receptor Inhibitors as Antifibrosis Agents.
Miwa S,Yokota M,Ueyama Y,Maeda K,Ogoshi Y,Seki N,Ogawa N,Nishihata J,Nomura A,Adachi T,Kitao Y,Nozawa K,Ishikawa T,Ukaji Y,Shiozaki M
ACS Med Chem Lett (2021) 12 : 745 -751
PubMed 34055221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.82 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4792978 1 6.75
CHEMBL4741913 1 6.72
CHEMBL4752199 1 6.51
CHEMBL4749011 1 6.28
CHEMBL4744988 1 6.20
CHEMBL4741185 1 6.16
CHEMBL4747422 1 6.10
CHEMBL4744618 1 6.07
CHEMBL4763122 1 6.02
CHEMBL4795223 1 5.96
CHEMBL4798505 1 5.92
CHEMBL4750258 1 5.92
CHEMBL4779579 1 5.89
CHEMBL4783244 1 5.89
CHEMBL4779273 1 5.72
CHEMBL4791414 1 5.64
CHEMBL4758580 1 5.64
CHEMBL4787891 1 5.62
CHEMBL4764416 1 5.57
CHEMBL4782729 1 5.54
CHEMBL4764221 1 5.54
CHEMBL4777071 1 5.52
CHEMBL4763627 1 5.52
CHEMBL4751832 1 5.52
CHEMBL4748097 1 5.42
CHEMBL4792464 1 5.39
CHEMBL4749061 1 5.28
CHEMBL4747912 1 4.70
CHEMBL4745367 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4792978 IC50 = 180.0 nM 6.75
CHEMBL4741913 IC50 = 190.0 nM 6.72
CHEMBL4752199 IC50 = 310.0 nM 6.51
CHEMBL4749011 IC50 = 530.0 nM 6.28
CHEMBL4744988 IC50 = 630.0 nM 6.20
CHEMBL4741185 IC50 = 700.0 nM 6.16
CHEMBL4747422 IC50 = 800.0 nM 6.10
CHEMBL4744618 IC50 = 860.0 nM 6.07
CHEMBL4763122 IC50 = 960.0 nM 6.02
CHEMBL4795223 IC50 = 1100.0 nM 5.96
CHEMBL4798505 IC50 = 1200.0 nM 5.92
CHEMBL4750258 IC50 = 1200.0 nM 5.92
CHEMBL4779579 IC50 = 1300.0 nM 5.89
CHEMBL4783244 IC50 = 1300.0 nM 5.89
CHEMBL4779273 IC50 = 1900.0 nM 5.72
CHEMBL4791414 IC50 = 2300.0 nM 5.64
CHEMBL4758580 IC50 = 2300.0 nM 5.64
CHEMBL4787891 IC50 = 2400.0 nM 5.62
CHEMBL4764416 IC50 = 2700.0 nM 5.57
CHEMBL4782729 IC50 = 2900.0 nM 5.54
CHEMBL4764221 IC50 = 2900.0 nM 5.54
CHEMBL4777071 IC50 = 3000.0 nM 5.52
CHEMBL4763627 IC50 = 3000.0 nM 5.52
CHEMBL4751832 IC50 = 3000.0 nM 5.52
CHEMBL4748097 IC50 = 3800.0 nM 5.42
CHEMBL4792464 IC50 = 4100.0 nM 5.39
CHEMBL4749061 IC50 = 5300.0 nM 5.28
CHEMBL4747912 IC50 = 20000.0 nM 4.70
CHEMBL4745367 IC50 > 20000.0 nM -