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Assay Detail

CHEMBL2390525

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Binding
Inhibition of ALK3 (unknown origin)
11
Total Activities
11
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

Bone morphogenetic protein receptor type-1A (CHEMBL5275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR.
Bioorg Med Chem Lett (2013) 23 : 3248 -3252
PubMed 23639540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.01 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511563 1 8.17
CHEMBL2385579 1 7.98
CHEMBL2385600 1 7.39
CHEMBL2385586 1 7.26
CHEMBL478629 DORSOMORPHIN 1 7.02
CHEMBL2385591 1 6.27
CHEMBL502351 1 4.97
CHEMBL2385596 1 -
CHEMBL2385582 1 -
CHEMBL2385597 1 -
CHEMBL513147 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511563 IC50 = 6.78 nM 8.17
CHEMBL2385579 IC50 = 10.4 nM 7.98
CHEMBL2385600 IC50 = 41.0 nM 7.39
CHEMBL2385586 IC50 = 55.0 nM 7.26
CHEMBL478629 DORSOMORPHIN IC50 = 95.0 nM 7.02
CHEMBL2385591 IC50 = 539.0 nM 6.27
CHEMBL502351 IC50 = 10800.0 nM 4.97
CHEMBL2385596 IC50 < 5.0 nM -
CHEMBL2385582 IC50 < 5.0 nM -
CHEMBL2385597 IC50 < 5.0 nM -
CHEMBL513147 IC50 < 5.0 nM -