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Assay Detail

CHEMBL2168975

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

Functional
Neuroprotective activity in rat PC12 cells expressing SOD1 G93A mutant assessed as increase in cell viability after 48 hrs by CalceinAM-based fluorescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type PC-12
Confidence 1 — Organism
Curated By Autocuration

Target

PC-12 (CHEMBL612556)
Type CELL-LINE
Organism Rattus norvegicus

Publication

Substituted pyrazolones require N2 hydrogen bond donating ability to protect against cytotoxicity from protein aggregation of mutant superoxide dismutase 1.
Trippier PC, Benmohamed R, Kirsch DR, Silverman RB.
Bioorg Med Chem Lett (2012) 22 : 6647 -6650
PubMed 23021992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.29 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1939222 1 7.17
CHEMBL2165383 1 6.89
CHEMBL2165387 1 6.57
CHEMBL2165389 1 6.51
CHEMBL2165390 1 6.48
CHEMBL2165377 1 6.47
CHEMBL2165384 1 6.44
CHEMBL2165388 1 6.38
CHEMBL2165386 1 6.31
CHEMBL2165374 1 6.25
CHEMBL2165372 1 6.17
CHEMBL2165375 1 6.17
CHEMBL2165392 1 6.03
CHEMBL2165382 1 6.00
CHEMBL2165378 1 5.99
CHEMBL2165393 1 5.88
CHEMBL2165391 1 5.77
CHEMBL2165379 1 5.76
CHEMBL2165380 1 -
CHEMBL2165381 1 -
CHEMBL2165376 1 -
CHEMBL2165385 1 -
CHEMBL2165373 1 -
CHEMBL2165371 1 -
CHEMBL2165370 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1939222 EC50 = 67.0 nM 7.17
CHEMBL2165383 EC50 = 130.0 nM 6.89
CHEMBL2165387 EC50 = 270.0 nM 6.57
CHEMBL2165389 EC50 = 310.0 nM 6.51
CHEMBL2165390 EC50 = 330.0 nM 6.48
CHEMBL2165377 EC50 = 340.0 nM 6.47
CHEMBL2165384 EC50 = 360.0 nM 6.44
CHEMBL2165388 EC50 = 420.0 nM 6.38
CHEMBL2165386 EC50 = 490.0 nM 6.31
CHEMBL2165374 EC50 = 560.0 nM 6.25
CHEMBL2165372 EC50 = 670.0 nM 6.17
CHEMBL2165375 EC50 = 670.0 nM 6.17
CHEMBL2165392 EC50 = 930.0 nM 6.03
CHEMBL2165382 EC50 = 1000.0 nM 6.00
CHEMBL2165378 EC50 = 1030.0 nM 5.99
CHEMBL2165393 EC50 = 1320.0 nM 5.88
CHEMBL2165391 EC50 = 1710.0 nM 5.77
CHEMBL2165379 EC50 = 1730.0 nM 5.76
CHEMBL2165380 EC50 > 32000.0 nM -
CHEMBL2165381 EC50 > 32000.0 nM -
CHEMBL2165376 EC50 > 32000.0 nM -
CHEMBL2165385 EC50 > 32000.0 nM -
CHEMBL2165373 EC50 > 32000.0 nM -
CHEMBL2165371 EC50 > 32000.0 nM -
CHEMBL2165370 EC50 > 32000.0 nM -