BDBM379697 US9926281, Compound 255
SMILES C[C@H]1CN(CCN1c1cc(F)cc(F)c1)C(=O)CC[C@]1(NC(=O)NC1=O)C1CC1
InChI Key InChIKey=CMLVKUWQFZQPPS-YUNKPMOVSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 18 hits for monomerid = 379697
Affinity DataIC50: 23nMAssay Description:ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For the do...More data for this Ligand-Target Pair
3D Structure (crystal)TargetA disintegrin and metalloproteinase with thrombospondin motifs 13(Homo sapiens (Human))
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of ADAMTS13 (unknown origin)More data for this Ligand-Target Pair
TargetDisintegrin and metalloproteinase domain-containing protein 17(Homo sapiens (Human))
Galapagos
US Patent
Galapagos
US Patent
Affinity DataIC50: >2.00E+4nMAssay Description:TACE:The basis for the assay is the cleavage of the substrate 5FAM-LAQAVRSSSRK-5TAMRA (SEQ ID No 3) (Anaspec, custom 34891) by human TACE (R&D SYSTEM...More data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of the proteases human MMP1 was determined at REACTION BIOLOGY (Reaction Biology Corp. 1 Great Valley Parkway, Suite 2 Malvern, Pa. 19355,...More data for this Ligand-Target Pair
Affinity DataIC50: 123nMAssay Description:MMP2: Protocol 2: The basis for the assay is the cleavage of the substrate 390 MMP FRET substrate I (Anaspec, Catalog n#: AS-27076) by human MMP2 (R&...More data for this Ligand-Target Pair
Affinity DataIC50: >2.00E+4nMAssay Description:MMP-13:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP13 (Chemicon, Cat #CC06...More data for this Ligand-Target Pair
Affinity DataIC50: 3.23E+3nMAssay Description:MMP-14:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP14 (Biomol, Cat #SE-259...More data for this Ligand-Target Pair
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assayMore data for this Ligand-Target Pair
TargetA disintegrin and metalloproteinase with thrombospondin motifs 1(Homo sapiens (Human))
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: >3.46E+3nMAssay Description:Inhibition of human recombinant ADAMTS-1 (AA253 to 734) assessed as cleavage of fluorescent substrate using 5(6)-fluorescein-NH-AELQGRPISIAK-5(6)-TAM...More data for this Ligand-Target Pair
TargetA disintegrin and metalloproteinase with thrombospondin motifs 4(Homo sapiens (Human))
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: 156nMAssay Description:Inhibition of human recombinant ADAMTS-4 (AA1 to 520) assessed as cleavage of fluorescent substrate using as TBIS-1 substrate incubated for 180 mins ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.16E+3nMAssay Description:Inhibition of human recombinant MMP2 (AA34 to 660) assessed as cleavage of fluorescent substrate using 390 MMP FRET as substrate incubated for 30 min...More data for this Ligand-Target Pair
Affinity DataIC50: >3.20E+3nMAssay Description:Inhibition of human recombinant MMP14 (AA112 to 298) assessed as cleavage of fluorescent substrate using 390 MMP FRET as substrate incubated for 30 m...More data for this Ligand-Target Pair
TargetDisintegrin and metalloproteinase domain-containing protein 17(Homo sapiens (Human))
Galapagos
US Patent
Galapagos
US Patent
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of human recombinant TACE (AA34 to 660) assessed as cleavage of fluorescent substrate using 5FAM-LAQAVRSSSRK-5TAMRA as substrate by bioche...More data for this Ligand-Target Pair
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Mus musculus)
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: <1.50E+3nMAssay Description:Inhibition of ADAMTS-5 in C57BL/6 mouse femoral head cartilage assessed as reduction in IL-1alpha stimulated glycosaminoglycan release measured after...More data for this Ligand-Target Pair
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: 63nMAssay Description:Inhibition of full-length human ADAMTS-5 expressed in HEK293-6E cells using AGC incubated for 50 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrateMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrateMore data for this Ligand-Target Pair
TargetA disintegrin and metalloproteinase with thrombospondin motifs 5(Homo sapiens (Human))
Galapagos
Curated by ChEMBL
Galapagos
Curated by ChEMBL
Affinity DataIC50: 20nMAssay Description:ADAMTS-5:Protocol 2: The basis for the assay is the cleavage of the substrate TBIS-1 (5 FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMT...More data for this Ligand-Target Pair