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Assay Detail

CHEMBL864074

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Binding
Inhibitory activity against humanized rabbit Cathepsin K
ChEMBL ↗
41
Total Activities
40
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

Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K.
Crane SN, Black WC, Palmer JT, Davis DE, Setti E, Robichaud J, Paquet J, Oballa RM, Bayly CI, McKay DJ, Somoza JR, Chauret N, Seto C, Scheigetz J, Wesolowski G, Massé F, Desmarais S, Ouellet M.
J Med Chem (2006) 49 : 1066 -1079
PubMed 16451072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 7.39 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201782 — — 1 9.55
CHEMBL201914 — — 1 9.34
CHEMBL201479 — — 1 9.30
CHEMBL383612 — — 1 9.24
CHEMBL371545 — — 1 8.77
CHEMBL201178 — — 1 8.59
CHEMBL371954 — — 2 8.43
CHEMBL201957 — — 1 8.38
CHEMBL201415 — — 1 8.30
CHEMBL202103 — — 1 8.15
CHEMBL202050 — — 1 7.77
CHEMBL202542 — — 1 7.68
CHEMBL201784 — — 1 7.55
CHEMBL201045 — — 1 7.52
CHEMBL370832 — — 1 7.52
CHEMBL201955 — — 1 7.48
CHEMBL370139 — — 1 7.44
CHEMBL202117 — — 1 7.00
CHEMBL371664 — — 1 7.00
CHEMBL201478 — — 1 6.96
CHEMBL381481 — — 1 6.82
CHEMBL382158 — — 1 6.82
CHEMBL200993 — — 1 6.76
CHEMBL202061 — — 1 6.70
CHEMBL202096 — — 1 6.70
CHEMBL378384 — — 1 6.55
CHEMBL383625 — — 1 6.48
CHEMBL425582 — — 1 6.46
CHEMBL201165 — — 1 6.43
CHEMBL201920 — — 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201782 — IC50 = 0.28 nM 9.55
CHEMBL201914 — IC50 = 0.46 nM 9.34
CHEMBL201479 — IC50 = 0.5 nM 9.30
CHEMBL383612 — IC50 = 0.58 nM 9.24
CHEMBL371545 — IC50 = 1.7 nM 8.77
CHEMBL201178 — IC50 = 2.6 nM 8.59
CHEMBL371954 — IC50 = 3.7 nM 8.43
CHEMBL371954 — IC50 = 4.2 nM 8.38
CHEMBL201957 — IC50 = 4.2 nM 8.38
CHEMBL201415 — IC50 = 5.0 nM 8.30
CHEMBL202103 — IC50 = 7.1 nM 8.15
CHEMBL202050 — IC50 = 17.0 nM 7.77
CHEMBL202542 — IC50 = 21.0 nM 7.68
CHEMBL201784 — IC50 = 28.0 nM 7.55
CHEMBL201045 — IC50 = 30.0 nM 7.52
CHEMBL370832 — IC50 = 30.0 nM 7.52
CHEMBL201955 — IC50 = 33.0 nM 7.48
CHEMBL370139 — IC50 = 36.0 nM 7.44
CHEMBL202117 — IC50 = 100.0 nM 7.00
CHEMBL371664 — IC50 = 100.0 nM 7.00
CHEMBL201478 — IC50 = 110.0 nM 6.96
CHEMBL381481 — IC50 = 150.0 nM 6.82
CHEMBL382158 — IC50 = 150.0 nM 6.82
CHEMBL200993 — IC50 = 172.0 nM 6.76
CHEMBL202096 — IC50 = 200.0 nM 6.70
CHEMBL202061 — IC50 = 200.0 nM 6.70
CHEMBL378384 — IC50 = 280.0 nM 6.55
CHEMBL383625 — IC50 = 330.0 nM 6.48
CHEMBL425582 — IC50 = 350.0 nM 6.46
CHEMBL201165 — IC50 = 370.0 nM 6.43
CHEMBL201920 — IC50 = 410.0 nM 6.39
CHEMBL202004 — IC50 = 460.0 nM 6.34
CHEMBL202114 — IC50 = 480.0 nM 6.32
CHEMBL383447 — IC50 = 490.0 nM 6.31
CHEMBL201166 — IC50 = 700.0 nM 6.16
CHEMBL202524 — IC50 = 950.0 nM 6.02
CHEMBL202622 — IC50 = 990.0 nM 6.00
CHEMBL427377 — IC50 - — -
CHEMBL381135 — IC50 - — -
CHEMBL201733 — IC50 - — -
CHEMBL202554 — IC50 - — -