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Assay Detail

CHEMBL2213246

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Binding
Inhibition of cathepsin S using FR-aminoluciferin as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay
ChEMBL ↗
80
Total Activities
80
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cathepsin S (CHEMBL2954) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
Moss N, Xiong Z, Burke M, Cogan D, Gao DA, Haverty K, Heim-Riether A, Hickey ER, Nagaraja R, Netherton M, O'Shea K, Ramsden P, Schwartz R, Shih DT, Ward Y, Young E, Zhang Q.
Bioorg Med Chem Lett (2012) 22 : 7189 -7193
PubMed 23084902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 7.77 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2207565 — — 1 10.00
CHEMBL2207564 — — 1 10.00
CHEMBL2207562 — — 1 9.52
CHEMBL251327 — — 1 9.40
CHEMBL2207591 — — 1 9.30
CHEMBL2207563 — — 1 9.30
CHEMBL2207571 — — 1 9.22
CHEMBL2207570 — — 1 9.22
CHEMBL2207567 — — 1 9.15
CHEMBL2207587 — — 1 9.00
CHEMBL2207566 — — 1 9.00
CHEMBL2207568 — — 1 8.96
CHEMBL1236882 — — 1 8.82
CHEMBL2207560 — — 1 8.80
CHEMBL2207588 — — 1 8.74
CHEMBL2207590 — — 1 8.66
CHEMBL2207569 — — 1 8.64
CHEMBL249915 — — 1 8.60
CHEMBL2207592 — — 1 8.51
CHEMBL2207156 — — 1 8.49
CHEMBL2207593 — — 1 8.46
CHEMBL2207585 — — 1 8.38
CHEMBL2207586 — — 1 8.34
CHEMBL2207157 — — 1 8.31
CHEMBL2207151 — — 1 8.28
CHEMBL2207158 — — 1 8.27
CHEMBL2203326 — — 1 8.25
CHEMBL2207159 — — 1 8.24
CHEMBL2207160 — — 1 8.23
CHEMBL2207589 — — 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2207565 — IC50 = 0.1 nM 10.00
CHEMBL2207564 — IC50 = 0.1 nM 10.00
CHEMBL2207562 — IC50 = 0.3 nM 9.52
CHEMBL251327 — IC50 = 0.4 nM 9.40
CHEMBL2207591 — IC50 = 0.5 nM 9.30
CHEMBL2207563 — IC50 = 0.5 nM 9.30
CHEMBL2207571 — IC50 = 0.6 nM 9.22
CHEMBL2207570 — IC50 = 0.6 nM 9.22
CHEMBL2207567 — IC50 = 0.7 nM 9.15
CHEMBL2207587 — IC50 = 1.0 nM 9.00
CHEMBL2207566 — IC50 = 1.0 nM 9.00
CHEMBL2207568 — IC50 = 1.1 nM 8.96
CHEMBL1236882 — IC50 = 1.5 nM 8.82
CHEMBL2207560 — IC50 = 1.6 nM 8.80
CHEMBL2207588 — IC50 = 1.8 nM 8.74
CHEMBL2207590 — IC50 = 2.2 nM 8.66
CHEMBL2207569 — IC50 = 2.3 nM 8.64
CHEMBL249915 — IC50 = 2.5 nM 8.60
CHEMBL2207592 — IC50 = 3.1 nM 8.51
CHEMBL2207156 — IC50 = 3.2 nM 8.49
CHEMBL2207593 — IC50 = 3.5 nM 8.46
CHEMBL2207585 — IC50 = 4.2 nM 8.38
CHEMBL2207586 — IC50 = 4.6 nM 8.34
CHEMBL2207157 — IC50 = 4.9 nM 8.31
CHEMBL2207151 — IC50 = 5.2 nM 8.28
CHEMBL2207158 — IC50 = 5.4 nM 8.27
CHEMBL2203326 — IC50 = 5.6 nM 8.25
CHEMBL2207159 — IC50 = 5.7 nM 8.24
CHEMBL2207160 — IC50 = 5.9 nM 8.23
CHEMBL2207589 — IC50 = 8.8 nM 8.06
CHEMBL2207161 — IC50 = 8.8 nM 8.06
CHEMBL2207561 — IC50 = 9.0 nM 8.05
CHEMBL2207150 — IC50 = 10.0 nM 8.00
CHEMBL387191 — IC50 = 10.0 nM 8.00
CHEMBL2207162 — IC50 = 13.0 nM 7.89
CHEMBL2207574 — IC50 = 13.0 nM 7.89
CHEMBL2207163 — IC50 = 15.0 nM 7.82
CHEMBL2207164 — IC50 = 15.0 nM 7.82
CHEMBL2207559 — IC50 = 17.0 nM 7.77
CHEMBL2207165 — IC50 = 17.0 nM 7.77
CHEMBL2207166 — IC50 = 18.0 nM 7.75
CHEMBL2207167 — IC50 = 23.0 nM 7.64
CHEMBL2207572 — IC50 = 27.0 nM 7.57
CHEMBL2207152 — IC50 = 28.0 nM 7.55
CHEMBL2207168 — IC50 = 28.0 nM 7.55
CHEMBL2207169 — IC50 = 29.0 nM 7.54
CHEMBL2207170 — IC50 = 33.0 nM 7.48
CHEMBL2207153 — IC50 = 34.0 nM 7.47
CHEMBL2207171 — IC50 = 38.0 nM 7.42
CHEMBL2207172 — IC50 = 39.0 nM 7.41