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Assay Detail

CHEMBL3994501

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

Binding
Inhibition of SDHB in human U2OS cells over-expressing Bim assessed as inhibition of apoptosis preincubated for 1 hr followed by doxycyclin addition to induce Bim protein expression measured after 24 hrs by Cell Titer-Glo assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of Highly Potent 2-Sulfonyl-Pyrimidinyl Derivatives for Apoptosis Inhibition and Ischemia Treatment.
Li L, Jiang X, Huang S, Ying Z, Zhang Z, Pan C, Li S, Wang X, Zhang Z.
ACS Med Chem Lett (2017) 8 : 407 -412
PubMed 28435527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 6.29 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078870 1 9.38
CHEMBL4078220 1 8.85
CHEMBL4091379 1 7.60
CHEMBL4064603 1 7.57
CHEMBL4070501 1 7.24
CHEMBL4061878 1 7.18
CHEMBL4092330 1 7.16
CHEMBL4082074 1 7.03
CHEMBL4071549 1 6.96
CHEMBL4086114 1 6.79
CHEMBL4093871 1 6.67
CHEMBL4083596 1 6.60
CHEMBL4089942 1 6.59
CHEMBL4073188 1 6.55
CHEMBL4101603 1 6.44
CHEMBL1430895 1 6.13
CHEMBL4101046 1 6.09
CHEMBL4070722 1 5.95
CHEMBL4063455 1 5.94
CHEMBL4085084 1 5.94
CHEMBL4097841 1 5.84
CHEMBL4090123 1 5.80
CHEMBL4097672 1 5.74
CHEMBL1492648 1 5.66
CHEMBL4063532 1 5.46
CHEMBL4096202 1 5.46
CHEMBL4086039 1 5.45
CHEMBL4103147 1 5.40
CHEMBL4074296 1 5.39
CHEMBL4062092 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078870 EC50 = 0.42 nM 9.38
CHEMBL4078220 EC50 = 1.4 nM 8.85
CHEMBL4091379 EC50 = 25.0 nM 7.60
CHEMBL4064603 EC50 = 27.0 nM 7.57
CHEMBL4070501 EC50 = 57.0 nM 7.24
CHEMBL4061878 EC50 = 66.0 nM 7.18
CHEMBL4092330 EC50 = 69.0 nM 7.16
CHEMBL4082074 EC50 = 94.0 nM 7.03
CHEMBL4071549 EC50 = 110.0 nM 6.96
CHEMBL4086114 EC50 = 164.0 nM 6.79
CHEMBL4093871 EC50 = 216.0 nM 6.67
CHEMBL4083596 EC50 = 253.0 nM 6.60
CHEMBL4089942 EC50 = 257.0 nM 6.59
CHEMBL4073188 EC50 = 282.0 nM 6.55
CHEMBL4101603 EC50 = 364.0 nM 6.44
CHEMBL1430895 EC50 = 749.0 nM 6.13
CHEMBL4101046 EC50 = 817.0 nM 6.09
CHEMBL4070722 EC50 = 1135.0 nM 5.95
CHEMBL4063455 EC50 = 1143.0 nM 5.94
CHEMBL4085084 EC50 = 1157.0 nM 5.94
CHEMBL4097841 EC50 = 1428.0 nM 5.84
CHEMBL4090123 EC50 = 1591.0 nM 5.80
CHEMBL4097672 EC50 = 1821.0 nM 5.74
CHEMBL1492648 EC50 = 2201.0 nM 5.66
CHEMBL4063532 EC50 = 3489.0 nM 5.46
CHEMBL4096202 EC50 = 3487.0 nM 5.46
CHEMBL4086039 EC50 = 3516.0 nM 5.45
CHEMBL4103147 EC50 = 4000.0 nM 5.40
CHEMBL4074296 EC50 = 4060.0 nM 5.39
CHEMBL4062092 EC50 = 4207.0 nM 5.38
CHEMBL4100077 EC50 = 4477.0 nM 5.35
CHEMBL4078150 EC50 = 6355.0 nM 5.20
CHEMBL4104624 EC50 = 6642.0 nM 5.18
CHEMBL4103961 EC50 = 7033.0 nM 5.15
CHEMBL4088482 EC50 = 8756.0 nM 5.06
CHEMBL4080611 EC50 > 20000.0 nM -
CHEMBL4081324 EC50 > 20000.0 nM -
CHEMBL4105576 EC50 > 20000.0 nM -
CHEMBL4089190 EC50 > 20000.0 nM -
CHEMBL4068001 EC50 > 20000.0 nM -
CHEMBL4104840 EC50 > 20000.0 nM -
CHEMBL4067221 EC50 > 20000.0 nM -
CHEMBL4102499 EC50 > 20000.0 nM -