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Assay Detail

CHEMBL2051644

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

Binding
Inhibition of renin in cynomolgus monkey plasma
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca fascicularis
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Renin (CHEMBL2046264)
Type SINGLE PROTEIN
Organism Macaca fascicularis

Publication

Design and optimization of novel (2S,4S,5S)-5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxy-2-isopropylhexanamides as renin inhibitors.
Nakamura Y, Sugita C, Meguro M, Miyazaki S, Tamaki K, Takahashi M, Nagai Y, Nagayama T, Kato M, Suemune H, Nishi T.
Bioorg Med Chem Lett (2012) 22 : 4561 -4566
PubMed 22726934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2048703 1 8.70
CHEMBL2048707 1 8.30
CHEMBL2048564 1 8.28
CHEMBL2046465 1 8.19
CHEMBL2048579 1 8.15
CHEMBL2048571 1 8.15
CHEMBL2048706 1 8.10
CHEMBL2048702 1 8.05
CHEMBL2048566 1 8.01
CHEMBL2048563 1 8.00
CHEMBL2048704 1 7.96
CHEMBL2048575 1 7.96
CHEMBL2048577 1 7.92
CHEMBL2048567 1 7.72
CHEMBL2048573 1 7.64
CHEMBL2048570 1 7.62
CHEMBL2048574 1 7.60
CHEMBL2048705 1 7.60
CHEMBL2048580 1 7.55
CHEMBL2048576 1 7.52
CHEMBL2048569 1 7.52
CHEMBL2048701 1 7.48
CHEMBL2048568 1 7.31
CHEMBL2048572 1 7.24
CHEMBL2048578 1 7.05
CHEMBL2048565 1 6.06
CHEMBL2048561 1 5.55
CHEMBL2048562 1 5.52
CHEMBL2048560 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2048703 IC50 = 2.0 nM 8.70
CHEMBL2048707 IC50 = 5.0 nM 8.30
CHEMBL2048564 IC50 = 5.3 nM 8.28
CHEMBL2046465 IC50 = 6.4 nM 8.19
CHEMBL2048579 IC50 = 7.0 nM 8.15
CHEMBL2048571 IC50 = 7.0 nM 8.15
CHEMBL2048706 IC50 = 8.0 nM 8.10
CHEMBL2048702 IC50 = 9.0 nM 8.05
CHEMBL2048566 IC50 = 9.8 nM 8.01
CHEMBL2048563 IC50 = 10.0 nM 8.00
CHEMBL2048704 IC50 = 11.0 nM 7.96
CHEMBL2048575 IC50 = 11.0 nM 7.96
CHEMBL2048577 IC50 = 12.0 nM 7.92
CHEMBL2048567 IC50 = 19.0 nM 7.72
CHEMBL2048573 IC50 = 23.0 nM 7.64
CHEMBL2048570 IC50 = 24.0 nM 7.62
CHEMBL2048574 IC50 = 25.0 nM 7.60
CHEMBL2048705 IC50 = 25.0 nM 7.60
CHEMBL2048580 IC50 = 28.0 nM 7.55
CHEMBL2048576 IC50 = 30.0 nM 7.52
CHEMBL2048569 IC50 = 30.0 nM 7.52
CHEMBL2048701 IC50 = 33.0 nM 7.48
CHEMBL2048568 IC50 = 49.0 nM 7.31
CHEMBL2048572 IC50 = 58.0 nM 7.24
CHEMBL2048578 IC50 = 90.0 nM 7.05
CHEMBL2048565 IC50 = 875.0 nM 6.06
CHEMBL2048561 IC50 = 2800.0 nM 5.55
CHEMBL2048562 IC50 = 3000.0 nM 5.52
CHEMBL2048560 IC50 = 12500.0 nM 4.90