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Assay Detail

CHEMBL4015013

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

Binding
Inhibition of 6-carboxyfluorescein succinimidyl ester fluorescence tagged-Bid BH3 peptide (79 to 99 residues) binding to Mcl-1 (unknown origin) after 30 mins by fluorescence polarization assay
42
Total Activities
42
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 and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors.
Luan S, Ge Q, Chen Y, Dai M, Yang J, Li K, Liu D, Zhao L.
Bioorg Med Chem Lett (2017) 27 : 1943 -1948
PubMed 28343875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 5.82 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4105602 1 6.96
CHEMBL4062127 1 6.85
CHEMBL4082302 1 6.82
CHEMBL4071224 1 6.70
CHEMBL4097869 1 6.70
CHEMBL51483 GOSSYPOL 3.0 1 6.70
CHEMBL4070752 1 6.60
CHEMBL4081347 1 6.51
CHEMBL4098261 1 6.44
CHEMBL4067010 1 6.24
CHEMBL4094073 1 6.13
CHEMBL4088240 1 6.10
CHEMBL4094488 1 6.05
CHEMBL4100319 1 6.02
CHEMBL4073436 1 5.92
CHEMBL4101383 1 5.83
CHEMBL4097987 1 5.82
CHEMBL4090152 1 5.79
CHEMBL4066811 1 5.73
CHEMBL4083396 1 5.70
CHEMBL4090685 1 5.68
CHEMBL4060541 1 5.62
CHEMBL4098490 1 5.59
CHEMBL4082881 1 5.57
CHEMBL4098411 1 5.52
CHEMBL4079739 1 5.49
CHEMBL4060999 1 5.47
CHEMBL4095827 1 5.38
CHEMBL4088098 1 5.36
CHEMBL4085651 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4105602 Ki = 110.0 nM 6.96
CHEMBL4062127 Ki = 140.0 nM 6.85
CHEMBL4082302 Ki = 150.0 nM 6.82
CHEMBL4071224 Ki = 200.0 nM 6.70
CHEMBL4097869 Ki = 200.0 nM 6.70
CHEMBL51483 GOSSYPOL Ki = 200.0 nM 6.70
CHEMBL4070752 Ki = 250.0 nM 6.60
CHEMBL4081347 Ki = 310.0 nM 6.51
CHEMBL4098261 Ki = 360.0 nM 6.44
CHEMBL4067010 Ki = 570.0 nM 6.24
CHEMBL4094073 Ki = 740.0 nM 6.13
CHEMBL4088240 Ki = 800.0 nM 6.10
CHEMBL4094488 Ki = 890.0 nM 6.05
CHEMBL4100319 Ki = 950.0 nM 6.02
CHEMBL4073436 Ki = 1190.0 nM 5.92
CHEMBL4101383 Ki = 1490.0 nM 5.83
CHEMBL4097987 Ki = 1500.0 nM 5.82
CHEMBL4090152 Ki = 1630.0 nM 5.79
CHEMBL4066811 Ki = 1870.0 nM 5.73
CHEMBL4083396 Ki = 2000.0 nM 5.70
CHEMBL4090685 Ki = 2100.0 nM 5.68
CHEMBL4060541 Ki = 2380.0 nM 5.62
CHEMBL4098490 Ki = 2570.0 nM 5.59
CHEMBL4082881 Ki = 2680.0 nM 5.57
CHEMBL4098411 Ki = 3000.0 nM 5.52
CHEMBL4079739 Ki = 3240.0 nM 5.49
CHEMBL4060999 Ki = 3370.0 nM 5.47
CHEMBL4095827 Ki = 4130.0 nM 5.38
CHEMBL4088098 Ki = 4420.0 nM 5.36
CHEMBL4085651 Ki = 5380.0 nM 5.27
CHEMBL4103583 Ki = 7780.0 nM 5.11
CHEMBL4098921 Ki = 8190.0 nM 5.09
CHEMBL4079962 Ki = 9890.0 nM 5.00
CHEMBL4077796 Ki = 10260.0 nM 4.99
CHEMBL4071936 Ki = 11610.0 nM 4.93
CHEMBL4069226 Ki = 12530.0 nM 4.90
CHEMBL4090275 Ki = 12870.0 nM 4.89
CHEMBL4069515 Ki > 30000.0 nM -
CHEMBL4060001 Ki > 30000.0 nM -
CHEMBL4080386 Ki > 30000.0 nM -
CHEMBL4094171 Ki > 30000.0 nM -
CHEMBL4069674 Ki > 30000.0 nM -