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Assay Detail

CHEMBL4199878

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

Binding
Inhibition of recombinant human N-terminal 6His/flag-tagged BMP1 (121 to 721 residues) expressed in CHO cells using ((5-FAM)-ELIDQYDVQRDDSSDGSLED-K(5,6 TAMRA)-CONH2) as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bone morphogenetic protein 1 (CHEMBL3898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1.
Kallander LS, Washburn D, Hilfiker MA, Eidam HS, Lawhorn BG, Prendergast J, Fox R, Dowdell S, Manns S, Hoang T, Zhao S, Ye G, Hammond M, Holt DA, Roethke T, Hong X, Reid RA, Gampe R, Zhang H, Diaz E, Rendina AR, Quinn AM, Willette B.
ACS Med Chem Lett (2018) 9 : 736 -740
PubMed 30034610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.16 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204567 1 9.00
CHEMBL4202714 1 9.00
CHEMBL4207907 1 8.10
CHEMBL4202960 1 7.70
CHEMBL4202420 1 7.60
CHEMBL4207308 1 7.50
CHEMBL4206785 1 6.90
CHEMBL4218334 1 6.80
CHEMBL4218229 1 6.80
CHEMBL4211285 1 5.90
CHEMBL4205331 1 5.40
CHEMBL4215581 1 5.20
CHEMBL4211663 1 -
CHEMBL4202848 1 -
CHEMBL4209125 1 -
CHEMBL4214046 1 -
CHEMBL4205697 1 -
CHEMBL4218415 1 -
CHEMBL4212386 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204567 IC50 = 1.0 nM 9.00
CHEMBL4202714 IC50 = 1.0 nM 9.00
CHEMBL4207907 IC50 = 8.0 nM 8.10
CHEMBL4202960 IC50 = 20.0 nM 7.70
CHEMBL4202420 IC50 = 25.0 nM 7.60
CHEMBL4207308 IC50 = 32.0 nM 7.50
CHEMBL4206785 IC50 = 126.0 nM 6.90
CHEMBL4218334 IC50 = 160.0 nM 6.80
CHEMBL4218229 IC50 = 160.0 nM 6.80
CHEMBL4211285 IC50 = 1250.0 nM 5.90
CHEMBL4205331 IC50 = 4000.0 nM 5.40
CHEMBL4215581 IC50 = 6300.0 nM 5.20
CHEMBL4211663 IC50 > 10000.0 nM -
CHEMBL4202848 IC50 < 1.0 nM -
CHEMBL4209125 IC50 < 1.0 nM -
CHEMBL4214046 IC50 < 1.0 nM -
CHEMBL4205697 IC50 < 1.0 nM -
CHEMBL4218415 IC50 < 1.0 nM -
CHEMBL4212386 IC50 < 1.0 nM -