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Assay Detail

CHEMBL799889

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

Functional
Negative logarithm of inhibitory concentration against bone resorption
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Farnesyl pyrophosphate synthase (CHEMBL1782)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents.
Kotsikorou E, Oldfield E.
J Med Chem (2003) 46 : 2932 -2944
PubMed 12825934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 55 7.65 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID 4.0 1 9.62
CHEMBL100827 1 9.21
CHEMBL56073 1 8.98
CHEMBL301247 1 8.96
CHEMBL101886 1 8.89
CHEMBL101472 1 8.84
CHEMBL101230 1 8.78
CHEMBL100508 1 8.74
CHEMBL101207 1 8.71
CHEMBL54537 1 8.59
CHEMBL55464 1 8.57
CHEMBL98476 1 8.57
CHEMBL316913 1 8.55
CHEMBL101407 1 8.51
CHEMBL316844 1 8.49
CHEMBL100441 1 8.41
CHEMBL301244 1 8.41
CHEMBL53982 1 8.40
CHEMBL319519 1 8.39
CHEMBL100835 1 8.37
CHEMBL100830 1 8.32
CHEMBL98703 1 8.30
CHEMBL100335 1 8.29
CHEMBL317646 1 8.29
CHEMBL100295 1 8.21
CHEMBL101539 1 8.15
CHEMBL316663 1 8.00
CHEMBL318071 1 7.98
CHEMBL97911 1 7.75
CHEMBL102209 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID IC50 = 0.2399 nM 9.62
CHEMBL100827 IC50 = 0.618 nM 9.21
CHEMBL56073 IC50 = 1.047 nM 8.98
CHEMBL301247 IC50 = 1.102 nM 8.96
CHEMBL101886 IC50 = 1.288 nM 8.89
CHEMBL101472 IC50 = 1.445 nM 8.84
CHEMBL101230 IC50 = 1.66 nM 8.78
CHEMBL100508 IC50 = 1.816 nM 8.74
CHEMBL101207 IC50 = 1.972 nM 8.71
CHEMBL54537 IC50 = 2.594 nM 8.59
CHEMBL55464 IC50 = 2.692 nM 8.57
CHEMBL98476 IC50 = 2.692 nM 8.57
CHEMBL316913 IC50 = 2.818 nM 8.55
CHEMBL101407 IC50 = 3.119 nM 8.51
CHEMBL316844 IC50 = 3.251 nM 8.49
CHEMBL100441 IC50 = 3.89 nM 8.41
CHEMBL301244 IC50 = 3.917 nM 8.41
CHEMBL53982 IC50 = 3.981 nM 8.40
CHEMBL319519 IC50 = 4.074 nM 8.39
CHEMBL100835 IC50 = 4.266 nM 8.37
CHEMBL100830 IC50 = 4.819 nM 8.32
CHEMBL98703 IC50 = 5.0 nM 8.30
CHEMBL100335 IC50 = 5.129 nM 8.29
CHEMBL317646 IC50 = 5.129 nM 8.29
CHEMBL100295 IC50 = 6.152 nM 8.21
CHEMBL101539 IC50 = 7.079 nM 8.15
CHEMBL316663 IC50 = 10.07 nM 8.00
CHEMBL318071 IC50 = 10.47 nM 7.98
CHEMBL97911 IC50 = 17.78 nM 7.75
CHEMBL102209 IC50 = 17.99 nM 7.75
CHEMBL100232 IC50 = 18.2 nM 7.74
CHEMBL100831 IC50 = 18.2 nM 7.74
CHEMBL323300 IC50 = 18.45 nM 7.73
CHEMBL318861 IC50 = 23.99 nM 7.62
CHEMBL321075 IC50 = 39.36 nM 7.41
CHEMBL102185 IC50 = 49.43 nM 7.31
CHEMBL323299 IC50 = 50.82 nM 7.29
CHEMBL273286 IC50 = 55.85 nM 7.25
CHEMBL98787 IC50 = 64.57 nM 7.19
CHEMBL98211 IC50 = 66.68 nM 7.18
CHEMBL101717 IC50 = 72.11 nM 7.14
CHEMBL101647 IC50 = 157.4 nM 6.80
CHEMBL318504 IC50 = 185.35 nM 6.73
CHEMBL101716 IC50 = 246.04 nM 6.61
CHEMBL293116 IC50 = 346.74 nM 6.46
CHEMBL327756 IC50 = 599.79 nM 6.22
CHEMBL98080 IC50 = 632.41 nM 6.20
CHEMBL98629 IC50 = 732.82 nM 6.13
CHEMBL98083 IC50 = 885.12 nM 6.05
CHEMBL97920 IC50 = 1174.9 nM 5.93