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Assay Detail

CHEMBL5733630

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Binding
The FP assay: The FP assay was then adapted for HTS and used to screen a ˜120,000 member small molecule library for compounds that displaced the FP probe from the T4 binding of TTR. “Hits” were defined as compounds that induced at least 50% decrease in fluorescence polarization and demonstrated relative fluorescence between 70 and 130%. 200 compounds were designated as positive hits (0.167% hit rate). The 200 hits were then evaluated in a dose-response manner and their IC50 (compound concentration that resulted in 50% decrease in the FP signal) values were determined. The top 100 hits were then purchased and their IC50 was confirmed again in >10-point duplicate dose response FP assay.
ChEMBL ↗
99
Total Activities
33
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Identification of stabilizers of multimeric proteins
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.73 6.56
kon 33 - -
k_off 33 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3695459 — — 3 6.56
CHEMBL63323 NIFLUMIC ACID 2.0 3 6.54
CHEMBL3695460 — — 3 6.53
CHEMBL591504 — — 3 6.52
CHEMBL1581319 — — 3 6.48
CHEMBL1835582 — — 3 6.36
CHEMBL5827486 — — 3 6.30
CHEMBL1370838 — — 3 6.23
CHEMBL28 APIGENIN — 3 6.18
CHEMBL168276 3,5-DINITROCATECHOL (OR-486) — 3 6.13
CHEMBL1256291 — — 3 6.12
CHEMBL183906 — — 3 6.09
CHEMBL1348329 — — 3 6.08
CHEMBL3695463 — — 3 5.94
CHEMBL3695464 — — 3 5.88
CHEMBL3695465 — — 3 5.59
CHEMBL3695466 — — 3 5.58
CHEMBL3695467 — — 3 5.47
CHEMBL2094716 — — 3 5.43
CHEMBL3695468 — — 3 5.43
CHEMBL3695469 — — 3 5.41
CHEMBL3695470 — — 3 5.38
CHEMBL493923 — — 3 5.32
CHEMBL3695471 — — 3 5.31
CHEMBL3695472 — — 3 5.31
CHEMBL3695473 — — 3 5.27
CHEMBL3695474 — — 3 5.25
CHEMBL181852 — — 3 5.24
CHEMBL3695475 — — 3 5.06
CHEMBL3695476 — — 3 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3695459 — IC50 = 277.0 nM 6.56
CHEMBL63323 NIFLUMIC ACID IC50 = 289.0 nM 6.54
CHEMBL3695460 — IC50 = 296.0 nM 6.53
CHEMBL591504 — IC50 = 301.0 nM 6.52
CHEMBL1581319 — IC50 = 329.0 nM 6.48
CHEMBL1835582 — IC50 = 433.0 nM 6.36
CHEMBL5827486 — IC50 = 504.0 nM 6.30
CHEMBL1370838 — IC50 = 586.0 nM 6.23
CHEMBL28 APIGENIN IC50 = 653.0 nM 6.18
CHEMBL168276 3,5-DINITROCATECHOL (OR-486) IC50 = 741.0 nM 6.13
CHEMBL1256291 — IC50 = 755.0 nM 6.12
CHEMBL183906 — IC50 = 815.0 nM 6.09
CHEMBL1348329 — IC50 = 842.0 nM 6.08
CHEMBL3695463 — IC50 = 1152.0 nM 5.94
CHEMBL3695464 — IC50 = 1306.0 nM 5.88
CHEMBL3695465 — IC50 = 2585.0 nM 5.59
CHEMBL3695466 — IC50 = 2656.0 nM 5.58
CHEMBL3695467 — IC50 = 3349.0 nM 5.47
CHEMBL2094716 — IC50 = 3707.0 nM 5.43
CHEMBL3695468 — IC50 = 3742.0 nM 5.43
CHEMBL3695469 — IC50 = 3927.0 nM 5.41
CHEMBL3695470 — IC50 = 4217.0 nM 5.38
CHEMBL493923 — IC50 = 4786.0 nM 5.32
CHEMBL3695471 — IC50 = 4881.0 nM 5.31
CHEMBL3695472 — IC50 = 4933.0 nM 5.31
CHEMBL3695473 — IC50 = 5414.0 nM 5.27
CHEMBL3695474 — IC50 = 5604.0 nM 5.25
CHEMBL181852 — IC50 = 5803.0 nM 5.24
CHEMBL3695475 — IC50 = 8690.0 nM 5.06
CHEMBL3695476 — IC50 = 9764.0 nM 5.01
CHEMBL3695477 — IC50 = 10039.0 nM 5.00
CHEMBL3695478 — IC50 = 10552.0 nM 4.98
CHEMBL241657 — IC50 = 10957.0 nM 4.96
CHEMBL3695477 — k_off = - s-1 -
CHEMBL3695471 — kon = - — -
CHEMBL3695474 — kon = - — -
CHEMBL493923 — k_off = - s-1 -
CHEMBL3695466 — kon = - — -
CHEMBL3695469 — kon = - — -
CHEMBL241657 — k_off = - s-1 -
CHEMBL3695469 — k_off = - s-1 -
CHEMBL3695475 — kon = - — -
CHEMBL3695475 — k_off = - s-1 -
CHEMBL3695470 — kon = - — -
CHEMBL3695470 — k_off = - s-1 -
CHEMBL181852 — k_off = - s-1 -
CHEMBL3695478 — k_off = - s-1 -
CHEMBL3695478 — kon = - — -
CHEMBL493923 — kon = - — -
CHEMBL241657 — kon = - — -