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Assay Detail

CHEMBL975288

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Binding
Inhibition of human recombinant rennin in buffer assessed as accumulation of angiotensin 1 using human tetradecapeptide by immunoassay
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Renin (CHEMBL286) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.
Bezençon O, Bur D, Weller T, Richard-Bildstein S, Remen L, Sifferlen T, Corminboeuf O, Grisostomi C, Boss C, Prade L, Delahaye S, Treiber A, Strickner P, Binkert C, Hess P, Steiner B, Fischli W.
J Med Chem (2009) 52 : 3689 -3702
PubMed 19358611 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 8.72 10.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276275 — — 1 10.41
CHEMBL508205 — — 1 9.80
CHEMBL449638 — — 1 9.70
CHEMBL504443 — — 1 9.70
CHEMBL443192 — — 1 9.60
CHEMBL452147 — — 1 9.55
CHEMBL454732 — — 1 9.54
CHEMBL506268 — — 1 9.52
CHEMBL503443 — — 1 9.48
CHEMBL443718 — — 1 9.46
CHEMBL509903 — — 1 9.40
CHEMBL444146 — — 1 9.32
CHEMBL448175 — — 1 9.26
CHEMBL503710 — — 1 9.26
CHEMBL1639 ALISKIREN 4.0 1 9.22
CHEMBL447097 — — 1 9.21
CHEMBL505635 — — 1 9.17
CHEMBL443469 — — 1 9.11
CHEMBL475671 — — 1 9.10
CHEMBL500811 — — 1 9.10
CHEMBL507560 — — 1 9.08
CHEMBL503129 — — 1 9.00
CHEMBL508158 — — 1 9.00
CHEMBL509480 — — 1 8.85
CHEMBL454711 — — 1 8.85
CHEMBL449458 — — 1 8.82
CHEMBL449779 — — 1 8.82
CHEMBL501586 — — 1 8.80
CHEMBL452191 — — 1 8.74
CHEMBL446741 — — 1 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276275 — IC50 = 0.039 nM 10.41
CHEMBL508205 — IC50 = 0.16 nM 9.80
CHEMBL504443 — IC50 = 0.2 nM 9.70
CHEMBL449638 — IC50 = 0.2 nM 9.70
CHEMBL443192 — IC50 = 0.25 nM 9.60
CHEMBL452147 — IC50 = 0.28 nM 9.55
CHEMBL454732 — IC50 = 0.29 nM 9.54
CHEMBL506268 — IC50 = 0.3 nM 9.52
CHEMBL503443 — IC50 = 0.33 nM 9.48
CHEMBL443718 — IC50 = 0.35 nM 9.46
CHEMBL509903 — IC50 = 0.4 nM 9.40
CHEMBL444146 — IC50 = 0.48 nM 9.32
CHEMBL448175 — IC50 = 0.55 nM 9.26
CHEMBL503710 — IC50 = 0.55 nM 9.26
CHEMBL1639 ALISKIREN IC50 = 0.6 nM 9.22
CHEMBL447097 — IC50 = 0.62 nM 9.21
CHEMBL505635 — IC50 = 0.67 nM 9.17
CHEMBL443469 — IC50 = 0.77 nM 9.11
CHEMBL475671 — IC50 = 0.79 nM 9.10
CHEMBL500811 — IC50 = 0.8 nM 9.10
CHEMBL507560 — IC50 = 0.83 nM 9.08
CHEMBL503129 — IC50 = 1.0 nM 9.00
CHEMBL508158 — IC50 = 1.0 nM 9.00
CHEMBL509480 — IC50 = 1.4 nM 8.85
CHEMBL454711 — IC50 = 1.4 nM 8.85
CHEMBL449458 — IC50 = 1.5 nM 8.82
CHEMBL449779 — IC50 = 1.5 nM 8.82
CHEMBL501586 — IC50 = 1.6 nM 8.80
CHEMBL452191 — IC50 = 1.8 nM 8.74
CHEMBL446741 — IC50 = 2.3 nM 8.64
CHEMBL470882 — IC50 = 2.4 nM 8.62
CHEMBL451603 — IC50 = 2.9 nM 8.54
CHEMBL502200 — IC50 = 3.2 nM 8.49
CHEMBL449505 — IC50 = 4.6 nM 8.34
CHEMBL508748 — IC50 = 4.8 nM 8.32
CHEMBL470878 — IC50 = 4.9 nM 8.31
CHEMBL507083 — IC50 = 5.2 nM 8.28
CHEMBL500205 — IC50 = 5.2 nM 8.28
CHEMBL510822 — IC50 = 6.6 nM 8.18
CHEMBL504403 — IC50 = 6.8 nM 8.17
CHEMBL453778 — IC50 = 7.0 nM 8.15
CHEMBL467850 — IC50 = 7.7 nM 8.11
CHEMBL447651 — IC50 = 8.3 nM 8.08
CHEMBL447104 — IC50 = 8.5 nM 8.07
CHEMBL509242 — IC50 = 10.0 nM 8.00
CHEMBL501912 — IC50 = 13.0 nM 7.89
CHEMBL505760 — IC50 = 13.0 nM 7.89
CHEMBL502925 — IC50 = 16.0 nM 7.80
CHEMBL511054 — IC50 = 19.0 nM 7.72
CHEMBL510710 — IC50 = 38.0 nM 7.42