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Assay Detail

CHEMBL2390527

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

Binding
Inhibition of BMP4 in mouse C2C12BRA cells after 14 hrs by luciferase reporter gene assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bone morphogenetic protein 4 (CHEMBL2384894)
Type SINGLE PROTEIN
Organism Mus musculus

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 32 6.41 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385596 1 7.60
CHEMBL2385600 1 7.03
CHEMBL2385591 1 6.93
CHEMBL2385579 1 6.85
CHEMBL502351 1 6.82
CHEMBL2385588 1 6.61
CHEMBL2385585 1 6.38
CHEMBL2385595 1 6.28
CHEMBL2385581 1 6.28
CHEMBL2385592 1 5.58
CHEMBL2385578 1 5.34
CHEMBL2385403 1 5.17
CHEMBL2385589 1 -
CHEMBL2385587 1 -
CHEMBL2385584 1 -
CHEMBL2385583 1 -
CHEMBL2385580 1 -
CHEMBL2385577 1 -
CHEMBL2385576 1 -
CHEMBL2385575 1 -
CHEMBL2385574 1 -
CHEMBL454786 1 -
CHEMBL2385601 1 -
CHEMBL2385599 1 -
CHEMBL467142 1 -
CHEMBL2385594 1 -
CHEMBL2385586 1 -
CHEMBL2385582 1 -
CHEMBL511563 1 -
CHEMBL2385598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385596 IC50 = 25.2 nM 7.60
CHEMBL2385600 IC50 = 94.1 nM 7.03
CHEMBL2385591 IC50 = 117.0 nM 6.93
CHEMBL2385579 IC50 = 141.0 nM 6.85
CHEMBL502351 IC50 = 152.0 nM 6.82
CHEMBL2385588 IC50 = 246.0 nM 6.61
CHEMBL2385585 IC50 = 418.0 nM 6.38
CHEMBL2385595 IC50 = 523.0 nM 6.28
CHEMBL2385581 IC50 = 529.0 nM 6.28
CHEMBL2385592 IC50 = 2636.0 nM 5.58
CHEMBL2385578 IC50 = 4571.0 nM 5.34
CHEMBL2385403 IC50 = 6732.0 nM 5.17
CHEMBL2385593 IC50 - -
CHEMBL2385590 IC50 - -
CHEMBL2385589 IC50 - -
CHEMBL2385587 IC50 - -
CHEMBL2385584 IC50 - -
CHEMBL2385583 IC50 - -
CHEMBL2385580 IC50 - -
CHEMBL2385577 IC50 - -
CHEMBL2385576 IC50 - -
CHEMBL2385575 IC50 - -
CHEMBL2385574 IC50 - -
CHEMBL454786 IC50 - -
CHEMBL2385601 IC50 - -
CHEMBL2385599 IC50 - -
CHEMBL467142 IC50 - -
CHEMBL2385594 IC50 - -
CHEMBL2385586 IC50 < 1.0 nM -
CHEMBL2385582 IC50 < 1.0 nM -
CHEMBL511563 IC50 < 1.0 nM -
CHEMBL2385598 IC50 - -