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Assay Detail

CHEMBL3749463

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Binding
Inhibition of human p97 ATPase incubated for 15 mins by ADP Glo luminescence assay
ChEMBL ↗
64
Total Activities
64
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

Transitional endoplasmic reticulum ATPase (CHEMBL1075145) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083).
Zhou HJ, Wang J, Yao B, Wong S, Djakovic S, Kumar B, Rice J, Valle E, Soriano F, Menon MK, Madriaga A, Kiss von Soly S, Kumar A, Parlati F, Yakes FM, Shawver L, Le Moigne R, Anderson DJ, Rolfe M, Wustrow D.
J Med Chem (2015) 58 : 9480 -9497
PubMed 26565666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 6.57 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3747448 — — 1 8.22
CHEMBL3747513 CB-5083 1.0 1 7.96
CHEMBL3746179 — — 1 7.82
CHEMBL3747049 — — 1 7.64
CHEMBL3747647 — — 1 7.40
CHEMBL3696924 — — 1 7.37
CHEMBL3696915 — — 1 7.33
CHEMBL3696925 — — 1 7.17
CHEMBL3745888 — — 1 7.15
CHEMBL3746353 — — 1 7.12
CHEMBL3746650 — — 1 7.02
CHEMBL3747498 — — 1 7.01
CHEMBL3746000 — — 1 6.84
CHEMBL3696863 — — 1 6.84
CHEMBL3747075 — — 1 6.83
CHEMBL3696917 — — 1 6.82
CHEMBL3696861 — — 1 6.82
CHEMBL3696873 — — 1 6.75
CHEMBL3696896 — — 1 6.72
CHEMBL3747639 — — 1 6.67
CHEMBL3696879 — — 1 6.64
CHEMBL3696878 — — 1 6.63
CHEMBL3746787 — — 1 6.61
CHEMBL3746988 — — 1 6.52
CHEMBL3745805 — — 1 6.47
CHEMBL3696920 — — 1 6.43
CHEMBL3746833 — — 1 6.43
CHEMBL3746037 — — 1 6.37
CHEMBL3696916 — — 1 6.35
CHEMBL3747140 — — 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3747448 — IC50 = 6.0 nM 8.22
CHEMBL3747513 CB-5083 IC50 = 11.0 nM 7.96
CHEMBL3746179 — IC50 = 15.0 nM 7.82
CHEMBL3747049 — IC50 = 23.0 nM 7.64
CHEMBL3747647 — IC50 = 40.0 nM 7.40
CHEMBL3696924 — IC50 = 43.0 nM 7.37
CHEMBL3696915 — IC50 = 47.0 nM 7.33
CHEMBL3696925 — IC50 = 68.0 nM 7.17
CHEMBL3745888 — IC50 = 71.0 nM 7.15
CHEMBL3746353 — IC50 = 76.0 nM 7.12
CHEMBL3746650 — IC50 = 95.0 nM 7.02
CHEMBL3747498 — IC50 = 98.0 nM 7.01
CHEMBL3746000 — IC50 = 144.0 nM 6.84
CHEMBL3696863 — IC50 = 145.0 nM 6.84
CHEMBL3747075 — IC50 = 149.0 nM 6.83
CHEMBL3696917 — IC50 = 153.0 nM 6.82
CHEMBL3696861 — IC50 = 152.0 nM 6.82
CHEMBL3696873 — IC50 = 180.0 nM 6.75
CHEMBL3696896 — IC50 = 192.0 nM 6.72
CHEMBL3747639 — IC50 = 215.0 nM 6.67
CHEMBL3696879 — IC50 = 227.0 nM 6.64
CHEMBL3696878 — IC50 = 233.0 nM 6.63
CHEMBL3746787 — IC50 = 248.0 nM 6.61
CHEMBL3746988 — IC50 = 304.0 nM 6.52
CHEMBL3745805 — IC50 = 342.0 nM 6.47
CHEMBL3696920 — IC50 = 370.0 nM 6.43
CHEMBL3746833 — IC50 = 367.0 nM 6.43
CHEMBL3746037 — IC50 = 425.0 nM 6.37
CHEMBL3696916 — IC50 = 445.0 nM 6.35
CHEMBL3747140 — IC50 = 632.0 nM 6.20
CHEMBL3747371 — IC50 = 648.0 nM 6.19
CHEMBL3747138 — IC50 = 651.0 nM 6.19
CHEMBL3696926 — IC50 = 795.0 nM 6.10
CHEMBL3746912 — IC50 = 815.0 nM 6.09
CHEMBL3696867 — IC50 = 907.0 nM 6.04
CHEMBL3696887 — IC50 = 1068.0 nM 5.97
CHEMBL3747194 — IC50 = 2075.0 nM 5.68
CHEMBL3747511 — IC50 = 3000.0 nM 5.52
CHEMBL3696895 — IC50 = 3134.0 nM 5.50
CHEMBL3747600 — IC50 = 3912.0 nM 5.41
CHEMBL3747097 — IC50 = 3860.0 nM 5.41
CHEMBL3746629 — IC50 = 4832.0 nM 5.32
CHEMBL3747552 — IC50 = 8908.0 nM 5.05
CHEMBL3696880 — IC50 > 5000.0 nM -
CHEMBL3746879 — IC50 > 5000.0 nM -
CHEMBL3746701 — IC50 > 5000.0 nM -
CHEMBL3746907 — IC50 > 5000.0 nM -
CHEMBL3745761 — IC50 > 5000.0 nM -
CHEMBL3745800 — IC50 > 5000.0 nM -
CHEMBL3747425 — IC50 > 5000.0 nM -