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Assay Detail

CHEMBL5530428

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

Binding
Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay
36
Total Activities
36
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

Publication

BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor.
Meibom D, Wasnaire P, Beyer K, Broehl A, Cancho-Grande Y, Elowe N, Henninger K, Johannes S, Jungmann N, Krainz T, Lindner N, Maassen S, MacDonald B, Menshykau D, Mittendorf J, Sanchez G, Schaefer M, Stefan E, Torge A, Xing Y, Zubov D.
J Med Chem (2024) 67 : 2907 -2940
PubMed 38348661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.34 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571635 1 8.52
CHEMBL5574355 1 8.52
CHEMBL5595087 1 8.30
CHEMBL5567356 1 8.22
CHEMBL5572837 1 8.10
CHEMBL5589887 1 8.05
CHEMBL5590012 1 8.00
CHEMBL5082898 1 7.89
CHEMBL5574922 1 7.85
CHEMBL5592187 1 7.82
CHEMBL5563780 1 7.80
CHEMBL5568936 1 7.75
CHEMBL5592274 1 7.72
CHEMBL5595652 1 7.72
CHEMBL5086874 1 7.68
CHEMBL5092149 1 7.58
CHEMBL5077651 1 7.58
CHEMBL5562698 1 7.54
CHEMBL5591976 1 7.34
CHEMBL5085716 1 7.33
CHEMBL5570826 1 7.33
CHEMBL5569538 1 7.22
CHEMBL5085514 1 7.21
CHEMBL5572305 1 7.14
CHEMBL5569748 1 7.10
CHEMBL5567489 1 7.00
CHEMBL5086082 1 6.94
CHEMBL5076179 1 6.89
CHEMBL5073508 1 6.75
CHEMBL5082246 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571635 IC50 = 3.0 nM 8.52
CHEMBL5574355 IC50 = 3.0 nM 8.52
CHEMBL5595087 IC50 = 5.0 nM 8.30
CHEMBL5567356 IC50 = 6.0 nM 8.22
CHEMBL5572837 IC50 = 8.0 nM 8.10
CHEMBL5589887 IC50 = 9.0 nM 8.05
CHEMBL5590012 IC50 = 10.0 nM 8.00
CHEMBL5082898 IC50 = 13.0 nM 7.89
CHEMBL5574922 IC50 = 14.0 nM 7.85
CHEMBL5592187 IC50 = 15.0 nM 7.82
CHEMBL5563780 IC50 = 16.0 nM 7.80
CHEMBL5568936 IC50 = 18.0 nM 7.75
CHEMBL5592274 IC50 = 19.0 nM 7.72
CHEMBL5595652 IC50 = 19.0 nM 7.72
CHEMBL5086874 IC50 = 21.0 nM 7.68
CHEMBL5092149 IC50 = 26.0 nM 7.58
CHEMBL5077651 IC50 = 26.0 nM 7.58
CHEMBL5562698 IC50 = 29.0 nM 7.54
CHEMBL5591976 IC50 = 46.0 nM 7.34
CHEMBL5570826 IC50 = 47.0 nM 7.33
CHEMBL5085716 IC50 = 47.0 nM 7.33
CHEMBL5569538 IC50 = 60.0 nM 7.22
CHEMBL5085514 IC50 = 61.0 nM 7.21
CHEMBL5572305 IC50 = 72.0 nM 7.14
CHEMBL5569748 IC50 = 79.0 nM 7.10
CHEMBL5567489 IC50 = 99.0 nM 7.00
CHEMBL5086082 IC50 = 115.0 nM 6.94
CHEMBL5076179 IC50 = 129.0 nM 6.89
CHEMBL5073508 IC50 = 180.0 nM 6.75
CHEMBL5082246 IC50 = 230.0 nM 6.64
CHEMBL5593541 IC50 = 280.0 nM 6.55
CHEMBL5572058 IC50 = 580.0 nM 6.24
CHEMBL5570775 IC50 = 850.0 nM 6.07
CHEMBL5590568 IC50 = 910.0 nM 6.04
CHEMBL5574157 IC50 = 930.0 nM 6.03
CHEMBL5575127 IC50 = 2300.0 nM 5.64