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Assay Detail

CHEMBL681827

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

Functional
pIC50 value for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
45
Total Activities
45
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 45 4.71 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319144 MINODRONIC ACID 4.0 1 5.39
CHEMBL55140 1 5.36
CHEMBL294192 1 5.31
CHEMBL340034 1 5.28
CHEMBL434024 1 5.24
CHEMBL923 RISEDRONIC ACID 4.0 1 5.16
CHEMBL291736 1 5.13
CHEMBL56255 (PENTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 5.11
CHEMBL301247 1 5.11
CHEMBL56011 1 5.05
CHEMBL125887 1 5.00
CHEMBL294191 1 5.00
CHEMBL55608 (BUTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.99
CHEMBL54472 N-(HEXAMETHYLENEIMINO)METHYLENEBISPHOSPHONIC ACID 1 4.95
CHEMBL53950 INCADRONIC ACID 2.0 1 4.94
CHEMBL55959 1 4.92
CHEMBL55557 1 4.90
CHEMBL301065 1 4.84
CHEMBL299717 (PROPYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.74
CHEMBL301244 1 4.71
CHEMBL55886 1 4.67
CHEMBL58830 (CYCLOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.60
CHEMBL997 IBANDRONIC ACID 4.0 1 4.50
CHEMBL55856 (ISOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.40
CHEMBL56253 (CYCLOHEXYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.40
CHEMBL55352 (DIPROPYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.39
CHEMBL412889 (CYCLOOCTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.36
CHEMBL55812 OLPADRONIC ACID 2.0 1 4.33
CHEMBL870 ALENDRONIC ACID 4.0 1 4.27
CHEMBL54926 (CYCLOBUTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319144 MINODRONIC ACID IC50 = 4073.8 nM 5.39
CHEMBL55140 IC50 = 4365.16 nM 5.36
CHEMBL294192 IC50 = 4897.79 nM 5.31
CHEMBL340034 IC50 = 5248.07 nM 5.28
CHEMBL434024 IC50 = 5754.4 nM 5.24
CHEMBL923 RISEDRONIC ACID IC50 = 6918.31 nM 5.16
CHEMBL291736 IC50 = 7413.1 nM 5.13
CHEMBL56255 (PENTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 7762.47 nM 5.11
CHEMBL301247 IC50 = 7762.47 nM 5.11
CHEMBL56011 IC50 = 8912.51 nM 5.05
CHEMBL125887 IC50 = 10000.0 nM 5.00
CHEMBL294191 IC50 = 10000.0 nM 5.00
CHEMBL55608 (BUTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 10232.93 nM 4.99
CHEMBL54472 N-(HEXAMETHYLENEIMINO)METHYLENEBISPHOSPHONIC ACID IC50 = 11220.18 nM 4.95
CHEMBL53950 INCADRONIC ACID IC50 = 11481.54 nM 4.94
CHEMBL55959 IC50 = 12022.64 nM 4.92
CHEMBL55557 IC50 = 12589.25 nM 4.90
CHEMBL301065 IC50 = 14454.4 nM 4.84
CHEMBL299717 (PROPYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 18197.01 nM 4.74
CHEMBL301244 IC50 = 19498.45 nM 4.71
CHEMBL55886 IC50 = 21379.62 nM 4.67
CHEMBL58830 (CYCLOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 25118.86 nM 4.60
CHEMBL997 IBANDRONIC ACID IC50 = 31622.78 nM 4.50
CHEMBL56253 (CYCLOHEXYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 39810.72 nM 4.40
CHEMBL55856 (ISOPENTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 39810.72 nM 4.40
CHEMBL55352 (DIPROPYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 40738.03 nM 4.39
CHEMBL412889 (CYCLOOCTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 43651.58 nM 4.36
CHEMBL55812 OLPADRONIC ACID IC50 = 46773.51 nM 4.33
CHEMBL870 ALENDRONIC ACID IC50 = 53703.18 nM 4.27
CHEMBL54926 (CYCLOBUTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 56234.13 nM 4.25
CHEMBL834 PAMIDRONIC ACID IC50 = 61659.5 nM 4.21
CHEMBL55358 IC50 = 63095.73 nM 4.20
CHEMBL54537 IC50 = 63095.73 nM 4.20
CHEMBL52137 IC50 = 66069.34 nM 4.18
CHEMBL417549 (NONYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 66069.34 nM 4.18
CHEMBL299988 IC50 = 91201.08 nM 4.04
CHEMBL316844 IC50 = 97723.72 nM 4.01
CHEMBL417932 IC50 = 251188.64 nM -
CHEMBL54344 (DIETHYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 131825.67 nM -
CHEMBL299563 THIOMORPHOLINOMETHYLENEDIPHOSPHONIC ACID IC50 = 190546.07 nM -
CHEMBL298771 IC50 = 102329.3 nM -
CHEMBL55264 IC50 = 213796.21 nM -
CHEMBL55214 NERIDRONIC ACID IC50 = 194984.46 nM -
CHEMBL293522 IC50 = 229086.77 nM -
CHEMBL56556 IC50 = 398107.17 nM -