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Assay Detail

CHEMBL804789

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Binding
Inhibitory activity against human renin
ChEMBL ↗
48
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites.
Kaltenbronn JS, Hudspeth JP, Lunney EA, Michniewicz BM, Nicolaides ED, Repine JT, RoarK WH, Stier MA, Tinney FJ, Woo PK.
J Med Chem (1990) 33 : 838 -845
PubMed 2405159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 5.60 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085574 — — 1 8.24
CHEMBL423262 — — 1 7.66
CHEMBL354821 — — 1 7.21
CHEMBL167426 — — 1 7.05
CHEMBL424543 — — 1 6.82
CHEMBL354766 — — 1 6.70
CHEMBL167218 — — 1 6.50
CHEMBL435266 — — 1 6.33
CHEMBL353204 — — 1 6.28
CHEMBL352450 — — 1 6.20
CHEMBL355409 — — 1 6.19
CHEMBL168378 — — 1 6.11
CHEMBL352937 — — 2 5.92
CHEMBL435076 — — 1 5.89
CHEMBL354969 — — 1 5.85
CHEMBL168482 — — 1 5.82
CHEMBL422209 — — 1 5.70
CHEMBL353106 — — 1 5.68
CHEMBL433538 — — 1 5.43
CHEMBL165754 — — 1 5.42
CHEMBL354767 — — 1 5.42
CHEMBL168261 — — 1 5.42
CHEMBL168323 — — 1 5.40
CHEMBL168712 — — 1 5.38
CHEMBL169818 — — 1 5.36
CHEMBL169255 — — 1 5.27
CHEMBL435470 — — 1 5.25
CHEMBL168374 — — 1 5.19
CHEMBL168302 — — 1 5.19
CHEMBL167109 — — 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085574 — IC50 = 5.7 nM 8.24
CHEMBL423262 — IC50 = 22.0 nM 7.66
CHEMBL354821 — IC50 = 61.0 nM 7.21
CHEMBL167426 — IC50 = 90.0 nM 7.05
CHEMBL424543 — IC50 = 150.0 nM 6.82
CHEMBL354766 — IC50 = 200.0 nM 6.70
CHEMBL167218 — IC50 = 320.0 nM 6.50
CHEMBL435266 — IC50 = 470.0 nM 6.33
CHEMBL353204 — IC50 = 530.0 nM 6.28
CHEMBL352450 — IC50 = 630.0 nM 6.20
CHEMBL355409 — IC50 = 640.0 nM 6.19
CHEMBL168378 — IC50 = 780.0 nM 6.11
CHEMBL352937 — IC50 = 1200.0 nM 5.92
CHEMBL435076 — IC50 = 1300.0 nM 5.89
CHEMBL354969 — IC50 = 1400.0 nM 5.85
CHEMBL168482 — IC50 = 1500.0 nM 5.82
CHEMBL422209 — IC50 = 2000.0 nM 5.70
CHEMBL353106 — IC50 = 2100.0 nM 5.68
CHEMBL433538 — IC50 = 3700.0 nM 5.43
CHEMBL165754 — IC50 = 3800.0 nM 5.42
CHEMBL354767 — IC50 = 3800.0 nM 5.42
CHEMBL168261 — IC50 = 3800.0 nM 5.42
CHEMBL168323 — IC50 = 4000.0 nM 5.40
CHEMBL168712 — IC50 = 4200.0 nM 5.38
CHEMBL169818 — IC50 = 4400.0 nM 5.36
CHEMBL169255 — IC50 = 5400.0 nM 5.27
CHEMBL435470 — IC50 = 5600.0 nM 5.25
CHEMBL168302 — IC50 = 6500.0 nM 5.19
CHEMBL168374 — IC50 = 6500.0 nM 5.19
CHEMBL167109 — IC50 = 6700.0 nM 5.17
CHEMBL168714 — IC50 = 7000.0 nM 5.16
CHEMBL354856 — IC50 = 7400.0 nM 5.13
CHEMBL165755 — IC50 = 8400.0 nM 5.08
CHEMBL168819 — IC50 = 9200.0 nM 5.04
CHEMBL351621 — IC50 = 10000.0 nM 5.00
CHEMBL354147 — IC50 = 11000.0 nM 4.96
CHEMBL424536 — IC50 = 11000.0 nM 4.96
CHEMBL355085 — IC50 = 13000.0 nM 4.89
CHEMBL351622 — IC50 = 15000.0 nM 4.82
CHEMBL354023 — IC50 = 18000.0 nM 4.75
CHEMBL169023 — IC50 = 18000.0 nM 4.75
CHEMBL166550 — IC50 = 21000.0 nM 4.68
CHEMBL167204 — IC50 = 23000.0 nM 4.64
CHEMBL424354 — IC50 = 23000.0 nM 4.64
CHEMBL353412 — IC50 = 26000.0 nM 4.58
CHEMBL350359 — IC50 = 29000.0 nM 4.54
CHEMBL355625 — IC50 > 100000.0 nM -
CHEMBL352937 — IC50 > 100000.0 nM -