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Assay Detail

CHEMBL681824

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

Functional
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T-cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Quantitative structure-activity relationships for gammadelta T cell activation by bisphosphonates.
Sanders JM, Ghosh S, Chan JM, Meints G, Wang H, Raker AM, Song Y, Colantino A, Burzynska A, Kafarski P, Morita CT, Oldfield E.
J Med Chem (2004) 47 : 375 -384
PubMed 14711309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 4.66 5.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55140 1 5.31
CHEMBL434024 1 5.25
CHEMBL923 RISEDRONIC ACID 4.0 1 5.21
CHEMBL340034 1 5.14
CHEMBL319144 MINODRONIC ACID 4.0 1 5.10
CHEMBL98110 1 5.00
CHEMBL301247 1 4.92
CHEMBL54472 N-(HEXAMETHYLENEIMINO)METHYLENEBISPHOSPHONIC ACID 1 4.89
CHEMBL55608 (BUTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.89
CHEMBL55557 1 4.85
CHEMBL294192 1 4.85
CHEMBL53950 INCADRONIC ACID 2.0 1 4.82
CHEMBL294191 1 4.80
CHEMBL125887 1 4.80
CHEMBL291736 1 4.80
CHEMBL56011 1 4.72
CHEMBL55886 1 4.68
CHEMBL301244 1 4.64
CHEMBL125461 1 4.62
CHEMBL301065 1 4.62
CHEMBL55959 1 4.55
CHEMBL997 IBANDRONIC ACID 4.0 1 4.51
CHEMBL299717 (PROPYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.46
CHEMBL56255 (PENTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.39
CHEMBL55856 (ISOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.33
CHEMBL56253 (CYCLOHEXYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.33
CHEMBL870 ALENDRONIC ACID 4.0 1 4.28
CHEMBL58830 (CYCLOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.26
CHEMBL124647 1 4.20
CHEMBL124796 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55140 IC50 = 4900.0 nM 5.31
CHEMBL434024 IC50 = 5600.0 nM 5.25
CHEMBL923 RISEDRONIC ACID IC50 = 6200.0 nM 5.21
CHEMBL340034 IC50 = 7300.0 nM 5.14
CHEMBL319144 MINODRONIC ACID IC50 = 8000.0 nM 5.10
CHEMBL98110 IC50 = 10000.0 nM 5.00
CHEMBL301247 IC50 = 12000.0 nM 4.92
CHEMBL54472 N-(HEXAMETHYLENEIMINO)METHYLENEBISPHOSPHONIC ACID IC50 = 13000.0 nM 4.89
CHEMBL55608 (BUTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 13000.0 nM 4.89
CHEMBL55557 IC50 = 14000.0 nM 4.85
CHEMBL294192 IC50 = 14000.0 nM 4.85
CHEMBL53950 INCADRONIC ACID IC50 = 15000.0 nM 4.82
CHEMBL125887 IC50 = 16000.0 nM 4.80
CHEMBL291736 IC50 = 16000.0 nM 4.80
CHEMBL294191 IC50 = 16000.0 nM 4.80
CHEMBL56011 IC50 = 19000.0 nM 4.72
CHEMBL55886 IC50 = 21000.0 nM 4.68
CHEMBL301244 IC50 = 23000.0 nM 4.64
CHEMBL125461 IC50 = 24000.0 nM 4.62
CHEMBL301065 IC50 = 24000.0 nM 4.62
CHEMBL55959 IC50 = 28000.0 nM 4.55
CHEMBL997 IBANDRONIC ACID IC50 = 31000.0 nM 4.51
CHEMBL299717 (PROPYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 35000.0 nM 4.46
CHEMBL56255 (PENTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 41000.0 nM 4.39
CHEMBL56253 (CYCLOHEXYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 47000.0 nM 4.33
CHEMBL55856 (ISOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 47000.0 nM 4.33
CHEMBL870 ALENDRONIC ACID IC50 = 52000.0 nM 4.28
CHEMBL58830 (CYCLOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 55000.0 nM 4.26
CHEMBL124647 IC50 = 63000.0 nM 4.20
CHEMBL124796 IC50 = 67000.0 nM 4.17
CHEMBL331016 N-(HEPTAMETHYLENEIMINO)METHYLENEBISPHOSPHONIC ACID IC50 = 68000.0 nM 4.17
CHEMBL125706 IC50 = 72000.0 nM 4.14
CHEMBL55352 (DIPROPYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 83000.0 nM 4.08
CHEMBL125188 IC50 = 110000.0 nM -
CHEMBL127801 IC50 = 348000.0 nM -
CHEMBL127186 IC50 = 1648000.0 nM -
CHEMBL412889 (CYCLOOCTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 110000.0 nM -
CHEMBL124324 IC50 = 400000.0 nM -
CHEMBL54926 (CYCLOBUTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 127000.0 nM -
CHEMBL338622 IC50 = 2070000.0 nM -
CHEMBL55214 NERIDRONIC ACID IC50 = 503000.0 nM -
CHEMBL417932 IC50 = 19939000.0 nM -
CHEMBL127588 IC50 = 9015000.0 nM -
CHEMBL338917 IC50 = 2741000.0 nM -
CHEMBL298771 IC50 = 213000.0 nM -
CHEMBL299563 THIOMORPHOLINOMETHYLENEDIPHOSPHONIC ACID IC50 = 597000.0 nM -
CHEMBL834 PAMIDRONIC ACID IC50 = 941000.0 nM -
CHEMBL340090 IC50 = 103000.0 nM -
CHEMBL55358 IC50 = 110000.0 nM -
CHEMBL417549 (NONYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 169000.0 nM -