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Assay Detail

CHEMBL3871748

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

Binding
Inhibition of 5-FAM-QEDIIRNIARHLAQVGDSMDRSIPPG binding to Mcl-1 (unknown origin) preincubated for 30 mins followed by FAM-labeled peptide addition measured after 20 mins by fluorescence polarization assay
44
Total Activities
44
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

Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
Wan Y, Liu T, Li X, Chen C, Fang H.
Bioorg Med Chem (2017) 25 : 138 -152
PubMed 27810438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.21 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3962531 1 7.11
CHEMBL51483 GOSSYPOL 3.0 1 6.75
CHEMBL3908357 1 6.66
CHEMBL3972866 1 6.58
CHEMBL3918764 1 6.52
CHEMBL3899305 1 6.50
CHEMBL3965513 1 6.48
CHEMBL3901796 1 6.47
CHEMBL3910834 1 6.39
CHEMBL3919776 1 6.37
CHEMBL3892614 1 6.34
CHEMBL3952094 1 6.32
CHEMBL3901516 1 6.30
CHEMBL3956472 1 6.30
CHEMBL3953936 1 6.30
CHEMBL3735206 1 6.28
CHEMBL3945206 1 6.27
CHEMBL3945560 1 6.25
CHEMBL3735093 1 6.25
CHEMBL3890693 1 6.24
CHEMBL3736460 1 6.24
CHEMBL3985300 1 6.23
CHEMBL3736193 1 6.20
CHEMBL3899665 1 6.17
CHEMBL3928678 1 6.15
CHEMBL3893523 1 6.14
CHEMBL3892448 1 6.13
CHEMBL3980896 1 6.11
CHEMBL3917309 1 6.11
CHEMBL3927686 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3962531 Ki = 77.0 nM 7.11
CHEMBL51483 GOSSYPOL Ki = 180.0 nM 6.75
CHEMBL3908357 Ki = 220.0 nM 6.66
CHEMBL3972866 Ki = 260.0 nM 6.58
CHEMBL3918764 Ki = 300.0 nM 6.52
CHEMBL3899305 Ki = 320.0 nM 6.50
CHEMBL3965513 Ki = 330.0 nM 6.48
CHEMBL3901796 Ki = 340.0 nM 6.47
CHEMBL3910834 Ki = 410.0 nM 6.39
CHEMBL3919776 Ki = 430.0 nM 6.37
CHEMBL3892614 Ki = 460.0 nM 6.34
CHEMBL3952094 Ki = 480.0 nM 6.32
CHEMBL3901516 Ki = 500.0 nM 6.30
CHEMBL3953936 Ki = 500.0 nM 6.30
CHEMBL3956472 Ki = 500.0 nM 6.30
CHEMBL3735206 Ki = 530.0 nM 6.28
CHEMBL3945206 Ki = 540.0 nM 6.27
CHEMBL3945560 Ki = 560.0 nM 6.25
CHEMBL3735093 Ki = 560.0 nM 6.25
CHEMBL3890693 Ki = 580.0 nM 6.24
CHEMBL3736460 Ki = 580.0 nM 6.24
CHEMBL3985300 Ki = 590.0 nM 6.23
CHEMBL3736193 Ki = 630.0 nM 6.20
CHEMBL3899665 Ki = 680.0 nM 6.17
CHEMBL3928678 Ki = 710.0 nM 6.15
CHEMBL3893523 Ki = 720.0 nM 6.14
CHEMBL3892448 Ki = 740.0 nM 6.13
CHEMBL3980896 Ki = 780.0 nM 6.11
CHEMBL3917309 Ki = 780.0 nM 6.11
CHEMBL3927686 Ki = 770.0 nM 6.11
CHEMBL3927341 Ki = 800.0 nM 6.10
CHEMBL3891727 Ki = 790.0 nM 6.10
CHEMBL3981494 Ki = 900.0 nM 6.05
CHEMBL3952775 Ki = 1300.0 nM 5.89
CHEMBL3961955 Ki = 2000.0 nM 5.70
CHEMBL3911506 Ki = 4000.0 nM 5.40
CHEMBL3920440 Ki = 4700.0 nM 5.33
CHEMBL3909769 Ki = 8100.0 nM 5.09
CHEMBL3908716 Ki > 10000.0 nM -
CHEMBL3917665 Ki > 10000.0 nM -
CHEMBL3926300 Ki > 10000.0 nM -
CHEMBL3980936 Ki - -
CHEMBL3944023 Ki - -
CHEMBL3916061 Ki - -