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Assay Detail

CHEMBL868495

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of trypsin
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Palmer JT, Rydzewski RM, Mendonca RV, Sperandio D, Spencer JR, Hirschbein BL, Lohman J, Beltman J, Nguyen M, Liu L.
Bioorg Med Chem Lett (2006) 16 : 3434 -3439
PubMed 16644215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.09 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535163 1 6.92
CHEMBL558178 1 6.75
CHEMBL538574 1 6.72
CHEMBL211561 1 6.72
CHEMBL537868 1 6.66
CHEMBL534492 1 6.52
CHEMBL537647 1 6.42
CHEMBL537646 1 6.38
CHEMBL539086 1 6.32
CHEMBL558199 1 6.30
CHEMBL556994 1 6.20
CHEMBL535386 1 6.07
CHEMBL558763 1 6.06
CHEMBL539088 1 5.96
CHEMBL559161 1 5.96
CHEMBL536973 1 5.96
CHEMBL539603 1 5.94
CHEMBL535617 1 5.85
CHEMBL535836 1 5.77
CHEMBL557979 1 5.72
CHEMBL557987 1 5.66
CHEMBL536290 1 5.62
CHEMBL559184 1 5.59
CHEMBL536972 1 5.48
CHEMBL535385 1 5.42
CHEMBL538085 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535163 Ki = 120.0 nM 6.92
CHEMBL558178 Ki = 180.0 nM 6.75
CHEMBL538574 Ki = 190.0 nM 6.72
CHEMBL211561 Ki = 190.0 nM 6.72
CHEMBL537868 Ki = 220.0 nM 6.66
CHEMBL534492 Ki = 300.0 nM 6.52
CHEMBL537647 Ki = 380.0 nM 6.42
CHEMBL537646 Ki = 415.0 nM 6.38
CHEMBL539086 Ki = 480.0 nM 6.32
CHEMBL558199 Ki = 500.0 nM 6.30
CHEMBL556994 Ki = 625.0 nM 6.20
CHEMBL535386 Ki = 850.0 nM 6.07
CHEMBL558763 Ki = 870.0 nM 6.06
CHEMBL539088 Ki = 1100.0 nM 5.96
CHEMBL559161 Ki = 1100.0 nM 5.96
CHEMBL536973 Ki = 1100.0 nM 5.96
CHEMBL539603 Ki = 1150.0 nM 5.94
CHEMBL535617 Ki = 1400.0 nM 5.85
CHEMBL535836 Ki = 1700.0 nM 5.77
CHEMBL557979 Ki = 1900.0 nM 5.72
CHEMBL557987 Ki = 2200.0 nM 5.66
CHEMBL536290 Ki = 2400.0 nM 5.62
CHEMBL559184 Ki = 2550.0 nM 5.59
CHEMBL536972 Ki = 3300.0 nM 5.48
CHEMBL535385 Ki = 3800.0 nM 5.42
CHEMBL538085 Ki = 3900.0 nM 5.41