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Assay Detail

CHEMBL663316

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Binding
Inhibition of cathepsin K
13
Total Activities
13
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

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Marquis RW, Yamashita DS, Ru Y, LoCastro SM, Oh HJ, Erhard KF, DesJarlais RL, Head MS, Smith WW, Zhao B, Janson CA, Abdel-Meguid SS, Tomaszek TA, Levy MA, Veber DF.
J Med Chem (1998) 41 : 3563 -3567
PubMed 9733481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.02 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113724 1 9.30
CHEMBL100563 1 8.64
CHEMBL118449 1 8.59
CHEMBL119285 1 8.46
CHEMBL281540 1 7.66
CHEMBL432634 1 7.60
CHEMBL119219 1 7.52
CHEMBL404801 1 7.25
CHEMBL117054 1 6.05
CHEMBL267064 1 5.46
CHEMBL118347 1 5.09
CHEMBL117790 1 4.82
CHEMBL325379 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113724 Ki = 0.5 nM 9.30
CHEMBL100563 Ki = 2.3 nM 8.64
CHEMBL118449 Ki = 2.6 nM 8.59
CHEMBL119285 Ki = 3.5 nM 8.46
CHEMBL281540 Ki = 22.0 nM 7.66
CHEMBL432634 Ki = 25.0 nM 7.60
CHEMBL119219 Ki = 30.0 nM 7.52
CHEMBL404801 Ki = 56.0 nM 7.25
CHEMBL117054 Ki = 900.0 nM 6.05
CHEMBL267064 Ki = 3500.0 nM 5.46
CHEMBL118347 Ki = 8200.0 nM 5.09
CHEMBL117790 Ki = 15000.0 nM 4.82
CHEMBL325379 Ki = 16000.0 nM 4.80