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Assay Detail

CHEMBL801708

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Binding
In vitro inhibitory activity against human plasma renin
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, structure-activity, and molecular modeling studies of potent renin inhibitory peptides having N-terminal Nin-For-Trp (Ftr): angiotensinogen congeners modified by P1-P1' Phe-Phe, Sta, Leu psi[CH(OH)CH2]Val or leu psi[CH2NH]Val substitutions.
Sawyer TK, Pals DT, Mao B, Staples DJ, de Vaux AE, Maggiora LL, Affholter JA, Kati W, Duchamp D, Hester JB.
J Med Chem (1988) 31 : 18 -30
PubMed 3275777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.56 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419531 1 10.00
CHEMBL1790497 DITEKIREN 2.0 1 9.96
CHEMBL320414 1 9.51
CHEMBL275711 1 9.42
CHEMBL318388 1 9.28
CHEMBL216847 1 9.00
CHEMBL317280 1 8.80
CHEMBL100924 1 8.42
CHEMBL329933 1 8.17
CHEMBL407670 1 8.00
CHEMBL330412 1 7.85
CHEMBL437836 1 7.80
CHEMBL316921 1 7.68
CHEMBL329982 1 7.51
CHEMBL263739 1 6.30
CHEMBL415839 1 5.68
CHEMBL262208 1 5.30
CHEMBL316614 1 5.24
CHEMBL413534 RIP 1 5.10
CHEMBL265165 1 5.08
CHEMBL296588 PEPSTATIN 2.0 1 4.66
CHEMBL436895 1 -
CHEMBL217629 1 -
CHEMBL420276 1 -
CHEMBL2370339 1 -
CHEMBL437516 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419531 IC50 = 0.1 nM 10.00
CHEMBL1790497 DITEKIREN IC50 = 0.11 nM 9.96
CHEMBL320414 IC50 = 0.31 nM 9.51
CHEMBL275711 IC50 = 0.38 nM 9.42
CHEMBL318388 IC50 = 0.53 nM 9.28
CHEMBL216847 IC50 = 1.0 nM 9.00
CHEMBL317280 IC50 = 1.6 nM 8.80
CHEMBL100924 IC50 = 3.8 nM 8.42
CHEMBL329933 IC50 = 6.8 nM 8.17
CHEMBL407670 IC50 = 10.0 nM 8.00
CHEMBL330412 IC50 = 14.0 nM 7.85
CHEMBL437836 IC50 = 16.0 nM 7.80
CHEMBL316921 IC50 = 21.0 nM 7.68
CHEMBL329982 IC50 = 31.0 nM 7.51
CHEMBL263739 IC50 = 500.0 nM 6.30
CHEMBL415839 IC50 = 2100.0 nM 5.68
CHEMBL262208 IC50 = 5000.0 nM 5.30
CHEMBL316614 IC50 = 5800.0 nM 5.24
CHEMBL413534 RIP IC50 = 8000.0 nM 5.10
CHEMBL265165 IC50 = 8300.0 nM 5.08
CHEMBL296588 PEPSTATIN IC50 = 22000.0 nM 4.66
CHEMBL436895 IC50 > 100000.0 nM -
CHEMBL217629 IC50 > 100000.0 nM -
CHEMBL420276 IC50 ~ 100000.0 nM -
CHEMBL2370339 IC50 > 100000.0 nM -
CHEMBL437516 IC50 > 100000.0 nM -