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Assay Detail

CHEMBL4836057

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

Binding
Stabilization of AL patient derived full length fluorescein-labeled IGLV6-57 expressed in Escherichia coli BL21 (DE3) measured after 24 hrs by proteolysis coupled-fluorescence polarization assay
44
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

Target

Immunoglobulin lambda variable 6-57 (CHEMBL4739844)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent Coumarin-Based Kinetic Stabilizers of Amyloidogenic Immunoglobulin Light Chains Using Structure-Based Design.
Yan NL, Santos-Martins D, Nair R, Chu A, Wilson IA, Johnson KA, Forli S, Morgan GJ, Petrassi HM, Kelly JW.
J Med Chem (2021) 64 : 6273 -6299
PubMed 33939422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 6.32 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4874211 1 8.39
CHEMBL4866500 2 8.07
CHEMBL4870683 1 8.06
CHEMBL4856046 1 7.60
CHEMBL4848583 1 7.45
CHEMBL4859730 1 7.32
CHEMBL4866739 1 7.21
CHEMBL4854105 1 7.15
CHEMBL4855805 1 7.11
CHEMBL4862037 1 6.99
CHEMBL4856361 1 6.96
CHEMBL4849658 1 6.82
CHEMBL4858385 1 6.82
CHEMBL4846353 1 6.68
CHEMBL4850480 1 6.54
CHEMBL4872061 1 6.54
CHEMBL4855362 1 6.52
CHEMBL4848404 2 6.52
CHEMBL4871026 1 6.50
CHEMBL4867929 1 6.38
CHEMBL4859449 1 6.26
CHEMBL4875945 1 6.25
CHEMBL4877002 1 6.09
CHEMBL4871041 1 6.07
CHEMBL4854803 1 5.96
CHEMBL4861156 1 5.86
CHEMBL4860180 1 5.77
CHEMBL4849620 1 5.71
CHEMBL4878847 1 5.70
CHEMBL4879274 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4874211 EC50 = 4.1 nM 8.39
CHEMBL4866500 EC50 = 8.6 nM 8.07
CHEMBL4870683 EC50 = 8.8 nM 8.06
CHEMBL4866500 EC50 = 11.5 nM 7.94
CHEMBL4856046 EC50 = 25.2 nM 7.60
CHEMBL4848583 EC50 = 35.6 nM 7.45
CHEMBL4859730 EC50 = 48.1 nM 7.32
CHEMBL4866739 EC50 = 62.4 nM 7.21
CHEMBL4854105 EC50 = 71.1 nM 7.15
CHEMBL4855805 EC50 = 77.1 nM 7.11
CHEMBL4862037 EC50 = 103.0 nM 6.99
CHEMBL4856361 EC50 = 110.0 nM 6.96
CHEMBL4858385 EC50 = 150.0 nM 6.82
CHEMBL4849658 EC50 = 151.0 nM 6.82
CHEMBL4846353 EC50 = 207.0 nM 6.68
CHEMBL4872061 EC50 = 289.0 nM 6.54
CHEMBL4850480 EC50 = 292.0 nM 6.54
CHEMBL4855362 EC50 = 302.0 nM 6.52
CHEMBL4848404 EC50 = 299.0 nM 6.52
CHEMBL4871026 EC50 = 313.0 nM 6.50
CHEMBL4867929 EC50 = 415.0 nM 6.38
CHEMBL4848404 EC50 = 477.0 nM 6.32
CHEMBL4859449 EC50 = 551.0 nM 6.26
CHEMBL4875945 EC50 = 558.0 nM 6.25
CHEMBL4877002 EC50 = 816.0 nM 6.09
CHEMBL4871041 EC50 = 855.0 nM 6.07
CHEMBL4854803 EC50 = 1110.0 nM 5.96
CHEMBL4861156 EC50 = 1370.0 nM 5.86
CHEMBL4860180 EC50 = 1690.0 nM 5.77
CHEMBL4849620 EC50 = 1960.0 nM 5.71
CHEMBL4878847 EC50 = 2000.0 nM 5.70
CHEMBL4879274 EC50 = 2650.0 nM 5.58
CHEMBL4852917 EC50 = 2860.0 nM 5.54
CHEMBL4847400 EC50 = 2970.0 nM 5.53
CHEMBL315348 EC50 = 3240.0 nM 5.49
CHEMBL4877901 EC50 = 3970.0 nM 5.40
CHEMBL4859852 EC50 = 3960.0 nM 5.40
CHEMBL4875269 EC50 = 5280.0 nM 5.28
CHEMBL4854056 EC50 = 7890.0 nM 5.10
CHEMBL4879384 EC50 = 9700.0 nM 5.01
CHEMBL4854892 EC50 = 18000.0 nM 4.75
CHEMBL4851449 EC50 = 18803.0 nM 4.73
CHEMBL4848237 EC50 = 26003.0 nM 4.58
CHEMBL4856004 EC50 - -