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Assay Detail

CHEMBL702337

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Functional
Inhibition of LPS-stimulated TNF-alpha release in human whole blood
ChEMBL ↗
96
Total Activities
96
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Expert

Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Xue CB, Voss ME, Nelson DJ, Duan JJ, Cherney RJ, Jacobson IC, He X, Roderick J, Chen L, Corbett RL, Wang L, Meyer DT, Kennedy K, DeGradodagger WF, Hardman KD, Teleha CA, Jaffee BD, Liu RQ, Copeland RA, Covington MB, Christ DD, Trzaskos JM, Newton RC, Magolda RL, Wexler RR, Decicco CP.
J Med Chem (2001) 44 : 2636 -2660
PubMed 11472217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 96 6.34 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91636 — — 1 7.17
CHEMBL313082 — — 1 7.16
CHEMBL90727 — — 1 7.16
CHEMBL88284 — — 1 7.08
CHEMBL330513 — — 1 7.07
CHEMBL88656 — — 1 7.03
CHEMBL88445 — — 1 7.00
CHEMBL419865 — — 1 7.00
CHEMBL2115226 — — 1 6.96
CHEMBL330547 — — 1 6.92
CHEMBL431008 — — 1 6.92
CHEMBL90332 — — 1 6.92
CHEMBL312972 — — 1 6.89
CHEMBL88651 — — 1 6.89
CHEMBL89406 — — 1 6.89
CHEMBL88342 — — 1 6.85
CHEMBL88133 — — 1 6.82
CHEMBL316158 — — 1 6.82
CHEMBL315276 — — 1 6.80
CHEMBL86542 — — 1 6.77
CHEMBL315393 — — 1 6.75
CHEMBL89419 — — 1 6.72
CHEMBL89335 — — 1 6.70
CHEMBL88979 — — 1 6.70
CHEMBL89034 — — 1 6.70
CHEMBL89426 — — 1 6.70
CHEMBL315721 — — 1 6.70
CHEMBL315318 — — 1 6.70
CHEMBL330723 — — 1 6.70
CHEMBL327639 — — 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91636 — IC50 = 67.0 nM 7.17
CHEMBL313082 — IC50 = 70.0 nM 7.16
CHEMBL90727 — IC50 = 70.0 nM 7.16
CHEMBL88284 — IC50 = 83.0 nM 7.08
CHEMBL330513 — IC50 = 85.0 nM 7.07
CHEMBL88656 — IC50 = 94.0 nM 7.03
CHEMBL88445 — IC50 = 100.0 nM 7.00
CHEMBL419865 — IC50 = 100.0 nM 7.00
CHEMBL2115226 — IC50 = 110.0 nM 6.96
CHEMBL330547 — IC50 = 120.0 nM 6.92
CHEMBL431008 — IC50 = 120.0 nM 6.92
CHEMBL90332 — IC50 = 120.0 nM 6.92
CHEMBL89406 — IC50 = 130.0 nM 6.89
CHEMBL88651 — IC50 = 130.0 nM 6.89
CHEMBL312972 — IC50 = 130.0 nM 6.89
CHEMBL88342 — IC50 = 140.0 nM 6.85
CHEMBL88133 — IC50 = 150.0 nM 6.82
CHEMBL316158 — IC50 = 150.0 nM 6.82
CHEMBL315276 — IC50 = 160.0 nM 6.80
CHEMBL86542 — IC50 = 170.0 nM 6.77
CHEMBL315393 — IC50 = 180.0 nM 6.75
CHEMBL89419 — IC50 = 190.0 nM 6.72
CHEMBL330723 — IC50 = 200.0 nM 6.70
CHEMBL315318 — IC50 = 200.0 nM 6.70
CHEMBL315721 — IC50 = 200.0 nM 6.70
CHEMBL89426 — IC50 = 200.0 nM 6.70
CHEMBL88979 — IC50 = 200.0 nM 6.70
CHEMBL89335 — IC50 = 200.0 nM 6.70
CHEMBL89034 — IC50 = 200.0 nM 6.70
CHEMBL327639 — IC50 = 210.0 nM 6.68
CHEMBL88906 — IC50 = 220.0 nM 6.66
CHEMBL88520 — IC50 = 220.0 nM 6.66
CHEMBL92546 — IC50 = 240.0 nM 6.62
CHEMBL89137 — IC50 = 260.0 nM 6.58
CHEMBL91425 — IC50 = 270.0 nM 6.57
CHEMBL327677 — IC50 = 270.0 nM 6.57
CHEMBL89045 — IC50 = 280.0 nM 6.55
CHEMBL89755 — IC50 = 280.0 nM 6.55
CHEMBL89374 — IC50 = 300.0 nM 6.52
CHEMBL327831 — IC50 = 300.0 nM 6.52
CHEMBL330249 — IC50 = 300.0 nM 6.52
CHEMBL88351 — IC50 = 300.0 nM 6.52
CHEMBL314428 — IC50 = 300.0 nM 6.52
CHEMBL313936 — IC50 = 390.0 nM 6.41
CHEMBL2114232 — IC50 = 400.0 nM 6.40
CHEMBL91990 — IC50 = 400.0 nM 6.40
CHEMBL92535 — IC50 = 400.0 nM 6.40
CHEMBL316061 — IC50 = 420.0 nM 6.38
CHEMBL88373 — IC50 = 460.0 nM 6.34
CHEMBL313552 — IC50 = 480.0 nM 6.32