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Assay Detail

CHEMBL929264

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

Binding
Inhibition of ACE2
26
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiotensin-converting enzyme 2 (CHEMBL3736)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and selective phosphinic peptide inhibitors of angiotensin-converting enzyme 2.
Mores A, Matziari M, Beau F, Cuniasse P, Yiotakis A, Dive V.
J Med Chem (2008) 51 : 2216 -2226
PubMed 18324760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.74 9.89
IC50 1 9.36 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260273 2 9.89
CHEMBL409105 1 9.40
CHEMBL429844 ORE-1001 1.0 1 9.36
CHEMBL261423 2 9.15
CHEMBL261121 1 8.90
CHEMBL258698 1 8.28
CHEMBL410509 1 8.28
CHEMBL411942 1 8.19
CHEMBL411052 1 8.18
CHEMBL263663 1 8.15
CHEMBL409721 1 8.12
CHEMBL408182 1 6.66
CHEMBL260677 1 6.52
CHEMBL411298 1 6.52
CHEMBL408448 1 6.10
CHEMBL408705 1 6.04
CHEMBL409713 1 5.52
CHEMBL264665 1 5.10
CHEMBL258683 1 -
CHEMBL261033 1 -
CHEMBL405232 1 -
CHEMBL412123 1 -
CHEMBL405913 1 -
CHEMBL258464 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260273 Ki = 0.13 nM 9.89
CHEMBL260273 Ki = 0.35 nM 9.46
CHEMBL409105 Ki = 0.4 nM 9.40
CHEMBL429844 ORE-1001 IC50 = 0.44 nM 9.36
CHEMBL261423 Ki = 0.7 nM 9.15
CHEMBL261121 Ki = 1.25 nM 8.90
CHEMBL261423 Ki = 2.1 nM 8.68
CHEMBL258698 Ki = 5.2 nM 8.28
CHEMBL410509 Ki = 5.2 nM 8.28
CHEMBL411942 Ki = 6.5 nM 8.19
CHEMBL411052 Ki = 6.6 nM 8.18
CHEMBL263663 Ki = 7.0 nM 8.15
CHEMBL409721 Ki = 7.5 nM 8.12
CHEMBL408182 Ki = 220.0 nM 6.66
CHEMBL260677 Ki = 300.0 nM 6.52
CHEMBL411298 Ki = 300.0 nM 6.52
CHEMBL408448 Ki = 800.0 nM 6.10
CHEMBL408705 Ki = 920.0 nM 6.04
CHEMBL409713 Ki = 3000.0 nM 5.52
CHEMBL264665 Ki = 8000.0 nM 5.10
CHEMBL258683 Ki > 10000.0 nM -
CHEMBL261033 Ki > 10000.0 nM -
CHEMBL405232 Ki > 10000.0 nM -
CHEMBL412123 Ki > 10000.0 nM -
CHEMBL405913 Ki > 10000.0 nM -
CHEMBL258464 Ki > 10000.0 nM -