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Assay Detail

CHEMBL808973

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Binding
Tested for inhibition against squalene synthase enzyme in rat liver
ChEMBL ↗
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Squalene synthase (CHEMBL3815) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives.
Ponpipom MM, Girotra NN, Bugianesi RL, Roberts CD, Berger GD, Burk RM, Marquis RW, Parsons WH, Bartizal KF, Bergstom JD.
J Med Chem (1994) 37 : 4031 -4051
PubMed 7966163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 8.72 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335394 — — 1 10.40
CHEMBL441322 — — 1 10.40
CHEMBL131147 — — 1 10.22
CHEMBL336939 — — 1 10.15
CHEMBL414430 — — 1 10.05
CHEMBL436588 — — 1 9.92
CHEMBL131335 — — 1 9.89
CHEMBL131201 — — 1 9.85
CHEMBL130959 — — 1 9.80
CHEMBL337434 — — 1 9.77
CHEMBL338582 — — 1 9.72
CHEMBL337256 — — 1 9.72
CHEMBL130431 — — 1 9.70
CHEMBL131604 — — 1 9.70
CHEMBL335456 — — 1 9.68
CHEMBL40991 ZARAGOZIC ACID A — 1 9.64
CHEMBL337266 — — 1 9.62
CHEMBL414247 — — 1 9.59
CHEMBL130435 — — 1 9.55
CHEMBL335691 — — 1 9.43
CHEMBL334791 — — 1 9.42
CHEMBL339013 — — 1 9.38
CHEMBL130767 — — 1 9.28
CHEMBL130012 — — 1 9.18
CHEMBL406872 — — 1 9.12
CHEMBL339362 — — 1 9.10
CHEMBL262441 — — 1 9.10
CHEMBL130218 — — 1 9.10
CHEMBL132100 — — 1 9.10
CHEMBL265327 — — 1 9.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335394 — IC50 = 0.04 nM 10.40
CHEMBL441322 — IC50 = 0.04 nM 10.40
CHEMBL131147 — IC50 = 0.06 nM 10.22
CHEMBL336939 — IC50 = 0.07 nM 10.15
CHEMBL414430 — IC50 = 0.09 nM 10.05
CHEMBL436588 — IC50 = 0.12 nM 9.92
CHEMBL131335 — IC50 = 0.13 nM 9.89
CHEMBL131201 — IC50 = 0.14 nM 9.85
CHEMBL130959 — IC50 = 0.16 nM 9.80
CHEMBL337434 — IC50 = 0.17 nM 9.77
CHEMBL338582 — IC50 = 0.19 nM 9.72
CHEMBL337256 — IC50 = 0.19 nM 9.72
CHEMBL131604 — IC50 = 0.2 nM 9.70
CHEMBL130431 — IC50 = 0.2 nM 9.70
CHEMBL335456 — IC50 = 0.21 nM 9.68
CHEMBL40991 ZARAGOZIC ACID A IC50 = 0.23 nM 9.64
CHEMBL337266 — IC50 = 0.24 nM 9.62
CHEMBL414247 — IC50 = 0.26 nM 9.59
CHEMBL130435 — IC50 = 0.28 nM 9.55
CHEMBL335691 — IC50 = 0.37 nM 9.43
CHEMBL334791 — IC50 = 0.38 nM 9.42
CHEMBL339013 — IC50 = 0.42 nM 9.38
CHEMBL130767 — IC50 = 0.52 nM 9.28
CHEMBL130012 — IC50 = 0.66 nM 9.18
CHEMBL406872 — IC50 = 0.75 nM 9.12
CHEMBL339362 — IC50 = 0.8 nM 9.10
CHEMBL132100 — IC50 = 0.8 nM 9.10
CHEMBL262441 — IC50 = 0.79 nM 9.10
CHEMBL130218 — IC50 = 0.8 nM 9.10
CHEMBL265327 — IC50 = 0.81 nM 9.09
CHEMBL337655 — IC50 = 1.0 nM 9.00
CHEMBL262677 — IC50 = 1.1 nM 8.96
CHEMBL337475 — IC50 = 1.2 nM 8.92
CHEMBL335710 — IC50 = 1.6 nM 8.80
CHEMBL334993 — IC50 = 1.8 nM 8.74
CHEMBL405288 — IC50 = 2.0 nM 8.70
CHEMBL336755 — IC50 = 2.0 nM 8.70
CHEMBL435200 — IC50 = 2.3 nM 8.64
CHEMBL335672 — IC50 = 3.0 nM 8.52
CHEMBL130003 — IC50 = 3.2 nM 8.49
CHEMBL131568 — IC50 = 3.4 nM 8.47
CHEMBL337432 — IC50 = 3.5 nM 8.46
CHEMBL131560 — IC50 = 4.3 nM 8.37
CHEMBL130532 — IC50 = 5.6 nM 8.25
CHEMBL423151 — IC50 = 8.0 nM 8.10
CHEMBL339319 — IC50 = 8.2 nM 8.09
CHEMBL131119 — IC50 = 8.8 nM 8.06
CHEMBL339460 — IC50 = 9.2 nM 8.04
CHEMBL133352 — IC50 = 9.2 nM 8.04
CHEMBL128770 — IC50 = 9.6 nM 8.02