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Assay Detail

CHEMBL3705320

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Binding
Enzyme Inhbition Assay: Enzyme activity is measured by observing the increase in fluorescence intensity caused by cleavage of a peptide substrate containing a fluorophore whose emission is quenched in the intact peptide.
ChEMBL ↗
86
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrrolidine derivatives
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 86 8.46 10.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3651506 — — 1 10.54
CHEMBL3651502 — — 1 10.28
CHEMBL3651507 — — 3 10.25
CHEMBL3651503 — — 2 10.25
CHEMBL3651508 — — 1 10.21
CHEMBL3651509 — — 1 9.96
CHEMBL3651505 — — 1 9.89
CHEMBL3651499 — — 1 9.82
CHEMBL3651510 — — 1 9.81
CHEMBL3651495 — — 1 9.78
CHEMBL3651493 — — 1 9.69
CHEMBL3651511 — — 1 9.52
CHEMBL3651473 — — 1 9.51
CHEMBL3651541 — — 1 9.49
CHEMBL3651497 — — 1 9.47
CHEMBL3651500 — — 1 9.45
CHEMBL3651498 — — 1 9.38
CHEMBL3651512 — — 1 9.30
CHEMBL3651496 — — 1 9.28
CHEMBL3651504 — — 1 9.27
CHEMBL3651494 — — 1 9.26
CHEMBL3651513 — — 1 9.20
CHEMBL3651481 — — 1 9.20
CHEMBL3651475 — — 1 9.19
CHEMBL3651514 — — 1 9.18
CHEMBL3651485 — — 1 9.18
CHEMBL3651486 — — 1 9.14
CHEMBL3651492 — — 1 9.05
CHEMBL3651483 — — 1 9.03
CHEMBL3651515 — — 1 9.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3651506 — IC50 = 0.029 nM 10.54
CHEMBL3651502 — IC50 = 0.052 nM 10.28
CHEMBL3651503 — IC50 = 0.056 nM 10.25
CHEMBL3651507 — IC50 = 0.056 nM 10.25
CHEMBL3651508 — IC50 = 0.061 nM 10.21
CHEMBL3651509 — IC50 = 0.11 nM 9.96
CHEMBL3651505 — IC50 = 0.13 nM 9.89
CHEMBL3651499 — IC50 = 0.15 nM 9.82
CHEMBL3651510 — IC50 = 0.155 nM 9.81
CHEMBL3651495 — IC50 = 0.167 nM 9.78
CHEMBL3651493 — IC50 = 0.205 nM 9.69
CHEMBL3651511 — IC50 = 0.305 nM 9.52
CHEMBL3651473 — IC50 = 0.31 nM 9.51
CHEMBL3651541 — IC50 = 0.32 nM 9.49
CHEMBL3651497 — IC50 = 0.335 nM 9.47
CHEMBL3651500 — IC50 = 0.355 nM 9.45
CHEMBL3651507 — IC50 = 0.365 nM 9.44
CHEMBL3651498 — IC50 = 0.415 nM 9.38
CHEMBL3651512 — IC50 = 0.5 nM 9.30
CHEMBL3651496 — IC50 = 0.52 nM 9.28
CHEMBL3651504 — IC50 = 0.535 nM 9.27
CHEMBL3651494 — IC50 = 0.55 nM 9.26
CHEMBL3651481 — IC50 = 0.63 nM 9.20
CHEMBL3651513 — IC50 = 0.63 nM 9.20
CHEMBL3651475 — IC50 = 0.65 nM 9.19
CHEMBL3651485 — IC50 = 0.665 nM 9.18
CHEMBL3651514 — IC50 = 0.66 nM 9.18
CHEMBL3651486 — IC50 = 0.73 nM 9.14
CHEMBL3651492 — IC50 = 0.883 nM 9.05
CHEMBL3651515 — IC50 = 0.945 nM 9.03
CHEMBL3651483 — IC50 = 0.935 nM 9.03
CHEMBL3651516 — IC50 = 1.2 nM 8.92
CHEMBL3651489 — IC50 = 1.433 nM 8.84
CHEMBL3651471 — IC50 = 1.5 nM 8.82
CHEMBL3651487 — IC50 = 1.5 nM 8.82
CHEMBL3651484 — IC50 = 1.65 nM 8.78
CHEMBL3651517 — IC50 = 1.7 nM 8.77
CHEMBL3651501 — IC50 = 1.7 nM 8.77
CHEMBL3651518 — IC50 = 1.8 nM 8.74
CHEMBL3651519 — IC50 = 2.121 nM 8.67
CHEMBL3651520 — IC50 = 2.202 nM 8.66
CHEMBL3651491 — IC50 = 2.3 nM 8.64
CHEMBL3651521 — IC50 = 2.35 nM 8.63
CHEMBL3651522 — IC50 = 2.7 nM 8.57
CHEMBL3651523 — IC50 = 2.75 nM 8.56
CHEMBL3651524 — IC50 = 3.15 nM 8.50
CHEMBL3651525 — IC50 = 3.2 nM 8.49
CHEMBL3651526 — IC50 = 3.55 nM 8.45
CHEMBL3651479 — IC50 = 3.6 nM 8.44
CHEMBL3651477 — IC50 = 4.0 nM 8.40