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Assay Detail

CHEMBL655960

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

Binding
50% inhibition of human C1r serine protease after 60 mins using Cbz-Gly-Arg-S-Bzl as substrate
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Complement C1r subcomponent (CHEMBL4611)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.
Hays SJ, Caprathe BW, Gilmore JL, Amin N, Emmerling MR, Michael W, Nadimpalli R, Nath R, Raser KJ, Stafford D, Watson D, Wang K, Jaen JC.
J Med Chem (1998) 41 : 1060 -1067
PubMed 9544206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.30 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274319 1 6.10
CHEMBL10252 1 6.05
CHEMBL10432 1 6.05
CHEMBL10610 1 6.05
CHEMBL10132 1 6.05
CHEMBL10248 1 5.82
CHEMBL274816 1 5.70
CHEMBL10435 1 5.55
CHEMBL10312 1 5.40
CHEMBL10527 1 5.38
CHEMBL10065 1 5.11
CHEMBL10050 1 5.10
CHEMBL276438 1 4.83
CHEMBL274211 1 4.82
CHEMBL10768 1 4.78
CHEMBL10770 1 4.78
CHEMBL10396 1 4.42
CHEMBL10117 1 4.33
CHEMBL10378 1 4.30
CHEMBL10554 1 -
CHEMBL10716 1 -
CHEMBL10254 1 -
CHEMBL10276 1 -
CHEMBL10757 1 -
CHEMBL10246 1 -
CHEMBL274137 1 -
CHEMBL10569 1 -
CHEMBL276464 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274319 IC50 = 800.0 nM 6.10
CHEMBL10252 IC50 = 900.0 nM 6.05
CHEMBL10432 IC50 = 900.0 nM 6.05
CHEMBL10610 IC50 = 900.0 nM 6.05
CHEMBL10132 IC50 = 900.0 nM 6.05
CHEMBL10248 IC50 = 1500.0 nM 5.82
CHEMBL274816 IC50 = 2000.0 nM 5.70
CHEMBL10435 IC50 = 2800.0 nM 5.55
CHEMBL10312 IC50 = 4000.0 nM 5.40
CHEMBL10527 IC50 = 4200.0 nM 5.38
CHEMBL10065 IC50 = 7800.0 nM 5.11
CHEMBL10050 IC50 = 8000.0 nM 5.10
CHEMBL276438 IC50 = 14700.0 nM 4.83
CHEMBL274211 IC50 = 15200.0 nM 4.82
CHEMBL10768 IC50 = 16600.0 nM 4.78
CHEMBL10770 IC50 = 16600.0 nM 4.78
CHEMBL10396 IC50 = 38000.0 nM 4.42
CHEMBL10117 IC50 = 47000.0 nM 4.33
CHEMBL10378 IC50 = 50000.0 nM 4.30
CHEMBL10554 IC50 > 62500.0 nM -
CHEMBL10716 IC50 > 62500.0 nM -
CHEMBL10254 IC50 > 62500.0 nM -
CHEMBL10276 IC50 > 62500.0 nM -
CHEMBL10757 IC50 > 62500.0 nM -
CHEMBL10246 IC50 > 62500.0 nM -
CHEMBL274137 IC50 > 62500.0 nM -
CHEMBL10569 IC50 > 62500.0 nM -
CHEMBL276464 IC50 > 62500.0 nM -