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Assay Detail

CHEMBL4836550

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

Binding
Binding affinity to 6His-Thr-BRD4 (1 to 477 residues) BD1 domain Y97A mutant (unknown origin) incubated for 30 mins by TR-FRET assay
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J, Gordon L, Grandi P, Gray JRJ, Harrison LA, Kruger RG, Matteo JJ, McCabe MT, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A, Zhang XP, Demont EH.
J Med Chem (2021) 64 : 10772 -10805
PubMed 34255512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 4.63 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297454 ABBV-744 1.0 1 6.40
CHEMBL4865712 — — 1 5.30
CHEMBL4858623 — — 1 5.00
CHEMBL4644310 — — 1 4.90
CHEMBL4635134 GSK620 — 1 4.80
CHEMBL4868843 — — 1 4.80
CHEMBL4874849 — — 1 4.80
CHEMBL4873541 — — 1 4.80
CHEMBL4648431 — — 1 4.70
CHEMBL4856380 — — 1 4.70
CHEMBL4847465 — — 1 4.70
CHEMBL4851297 — — 1 4.70
CHEMBL4858822 — — 1 4.60
CHEMBL4873141 — — 1 4.60
CHEMBL4637208 GSK973 — 1 4.60
CHEMBL4865767 — — 1 4.60
CHEMBL4860153 — — 1 4.60
CHEMBL4864363 — — 1 4.50
CHEMBL4874570 — — 1 4.50
CHEMBL4869293 — — 1 4.50
CHEMBL4852373 — — 1 4.50
CHEMBL4873873 — — 1 4.50
CHEMBL4855898 — — 1 4.50
CHEMBL4866897 — — 1 4.50
CHEMBL4849681 — — 1 4.50
CHEMBL4858377 — — 1 4.50
CHEMBL4873842 — — 1 4.50
CHEMBL4858662 — — 1 4.40
CHEMBL4851248 — — 1 4.40
CHEMBL4862598 — — 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297454 ABBV-744 IC50 = 398.11 nM 6.40
CHEMBL4865712 — IC50 = 5011.87 nM 5.30
CHEMBL4858623 — IC50 = 10000.0 nM 5.00
CHEMBL4644310 — IC50 = 12589.25 nM 4.90
CHEMBL4635134 GSK620 IC50 = 15848.93 nM 4.80
CHEMBL4868843 — IC50 = 15848.93 nM 4.80
CHEMBL4874849 — IC50 = 15848.93 nM 4.80
CHEMBL4873541 — IC50 = 15848.93 nM 4.80
CHEMBL4851297 — IC50 = 19952.62 nM 4.70
CHEMBL4847465 — IC50 = 19952.62 nM 4.70
CHEMBL4856380 — IC50 = 19952.62 nM 4.70
CHEMBL4648431 — IC50 = 19952.62 nM 4.70
CHEMBL4860153 — IC50 = 25118.86 nM 4.60
CHEMBL4865767 — IC50 = 25118.86 nM 4.60
CHEMBL4637208 GSK973 IC50 = 25118.86 nM 4.60
CHEMBL4858822 — IC50 = 25118.86 nM 4.60
CHEMBL4873141 — IC50 = 25118.86 nM 4.60
CHEMBL4849681 — IC50 = 31622.78 nM 4.50
CHEMBL4873842 — IC50 = 31622.78 nM 4.50
CHEMBL4858377 — IC50 = 31622.78 nM 4.50
CHEMBL4866897 — IC50 = 31622.78 nM 4.50
CHEMBL4855898 — IC50 = 31622.78 nM 4.50
CHEMBL4852373 — IC50 = 31622.78 nM 4.50
CHEMBL4869293 — IC50 = 31622.78 nM 4.50
CHEMBL4874570 — IC50 = 31622.78 nM 4.50
CHEMBL4864363 — IC50 = 31622.78 nM 4.50
CHEMBL4873873 — IC50 = 31622.78 nM 4.50
CHEMBL4858662 — IC50 = 39810.72 nM 4.40
CHEMBL4851248 — IC50 = 39810.72 nM 4.40
CHEMBL4862598 — IC50 = 39810.72 nM 4.40
CHEMBL4858395 — IC50 = 39810.72 nM 4.40
CHEMBL4636881 GSK046 IC50 = 50118.72 nM 4.30
CHEMBL4852313 — IC50 = 50118.72 nM 4.30
CHEMBL4868396 — IC50 = 50118.72 nM 4.30
CHEMBL4846225 — IC50 = 50118.72 nM 4.30
CHEMBL4854042 — IC50 = 79432.82 nM 4.10
CHEMBL4876906 — IC50 > 50118.72 nM -
CHEMBL4869159 — IC50 > 50118.72 nM -
CHEMBL4866545 — IC50 > 50118.72 nM -
CHEMBL4850744 — IC50 > 50118.72 nM -
CHEMBL4860965 — IC50 > 50118.72 nM -
CHEMBL4875959 — IC50 > 50118.72 nM -
CHEMBL4847809 — IC50 > 50118.72 nM -
CHEMBL4857058 — IC50 > 50118.72 nM -
CHEMBL4862278 — IC50 > 50118.72 nM -
CHEMBL4865140 — IC50 > 50118.72 nM -
CHEMBL4853784 — IC50 > 50118.72 nM -
CHEMBL4870415 — IC50 > 50118.72 nM -
CHEMBL4878480 — IC50 > 50118.72 nM -