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Assay Detail

CHEMBL911374

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Binding
Inhibition of ADAM10
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Publication

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Yao W, Zhuo J, Burns DM, Xu M, Zhang C, Li YL, Qian DQ, He C, Weng L, Shi E, Lin Q, Agrios C, Burn TC, Caulder E, Covington MB, Fridman JS, Friedman S, Katiyar K, Hollis G, Li Y, Liu C, Liu X, Marando CA, Newton R, Pan M, Scherle P, Taylor N, Vaddi K, Wasserman ZR, Wynn R, Yeleswaram S, Jalluri R, Bower M, Zhou BB, Metcalf B.
J Med Chem (2007) 50 : 603 -606
PubMed 17256836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.86 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375418 1 7.64
CHEMBL373532 1 7.48
CHEMBL434567 1 7.23
CHEMBL219105 1 7.11
CHEMBL221698 1 7.01
CHEMBL221120 1 6.96
CHEMBL221857 1 6.92
CHEMBL373853 1 6.89
CHEMBL387202 1 6.51
CHEMBL219104 1 6.50
CHEMBL426388 1 6.48
CHEMBL221537 1 6.32
CHEMBL218586 1 6.14
CHEMBL220501 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375418 IC50 = 23.0 nM 7.64
CHEMBL373532 IC50 = 33.0 nM 7.48
CHEMBL434567 IC50 = 59.0 nM 7.23
CHEMBL219105 IC50 = 77.0 nM 7.11
CHEMBL221698 IC50 = 97.0 nM 7.01
CHEMBL221120 IC50 = 110.0 nM 6.96
CHEMBL221857 IC50 = 120.0 nM 6.92
CHEMBL373853 IC50 = 130.0 nM 6.89
CHEMBL387202 IC50 = 310.0 nM 6.51
CHEMBL219104 IC50 = 320.0 nM 6.50
CHEMBL426388 IC50 = 330.0 nM 6.48
CHEMBL221537 IC50 = 480.0 nM 6.32
CHEMBL218586 IC50 = 720.0 nM 6.14
CHEMBL220501 IC50 > 5000.0 nM -