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Assay Detail

CHEMBL4809907

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

Binding
Displacement of Alexa Fluor 647 labelled ligand from 6His-Thr tagged BRD4 BD2/BD1 Y97A mutant (1 to 477 residue) (unknown origin) measured after 30 mins by TR-FRET assay
ChEMBL ↗
43
Total Activities
43
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

Bromodomain-containing protein 4 (CHEMBL1163125) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a Series of <i>N</i>-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
Harrison LA, Atkinson SJ, Bassil A, Chung CW, Grandi P, Gray JRJ, Levernier E, Lewis A, Lugo D, Messenger C, Michon AM, Mitchell DJ, Preston A, Prinjha RK, Rioja I, Seal JT, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH.
J Med Chem (2021) 64 : 10742 -10771
PubMed 34232650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 7.03 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846199 — — 1 8.00
CHEMBL4873182 — — 1 8.00
CHEMBL4862372 — — 1 7.90
CHEMBL4860220 — — 1 7.80
CHEMBL4648431 — — 1 7.80
CHEMBL4865699 — — 1 7.70
CHEMBL4846439 — — 1 7.70
CHEMBL4863255 — — 1 7.70
CHEMBL4850783 — — 1 7.60
CHEMBL4857098 — — 1 7.60
CHEMBL4867556 — — 1 7.50
CHEMBL4863388 — — 1 7.50
CHEMBL4854638 — — 1 7.40
CHEMBL4861058 — — 1 7.40
CHEMBL4875717 — — 1 7.40
CHEMBL4877086 — — 1 7.40
CHEMBL4868170 — — 1 7.40
CHEMBL4849578 — — 1 7.40
CHEMBL4636881 GSK046 — 1 7.30
CHEMBL4852357 — — 1 7.30
CHEMBL4873988 — — 1 7.30
CHEMBL4861542 — — 1 7.30
CHEMBL4867905 — — 1 7.20
CHEMBL4858519 — — 1 7.20
CHEMBL4871681 — — 1 7.20
CHEMBL4849259 — — 1 7.10
CHEMBL4635134 GSK620 — 1 7.10
CHEMBL4644310 — — 1 7.10
CHEMBL4866464 — — 1 7.00
CHEMBL4876311 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846199 — IC50 = 10.0 nM 8.00
CHEMBL4873182 — IC50 = 10.0 nM 8.00
CHEMBL4862372 — IC50 = 12.59 nM 7.90
CHEMBL4860220 — IC50 = 15.85 nM 7.80
CHEMBL4648431 — IC50 = 15.85 nM 7.80
CHEMBL4865699 — IC50 = 19.95 nM 7.70
CHEMBL4846439 — IC50 = 19.95 nM 7.70
CHEMBL4863255 — IC50 = 19.95 nM 7.70
CHEMBL4850783 — IC50 = 25.12 nM 7.60
CHEMBL4857098 — IC50 = 25.12 nM 7.60
CHEMBL4867556 — IC50 = 31.62 nM 7.50
CHEMBL4863388 — IC50 = 31.62 nM 7.50
CHEMBL4849578 — IC50 = 39.81 nM 7.40
CHEMBL4868170 — IC50 = 39.81 nM 7.40
CHEMBL4877086 — IC50 = 39.81 nM 7.40
CHEMBL4854638 — IC50 = 39.81 nM 7.40
CHEMBL4875717 — IC50 = 39.81 nM 7.40
CHEMBL4861058 — IC50 = 39.81 nM 7.40
CHEMBL4861542 — IC50 = 50.12 nM 7.30
CHEMBL4873988 — IC50 = 50.12 nM 7.30
CHEMBL4636881 GSK046 IC50 = 50.12 nM 7.30
CHEMBL4852357 — IC50 = 50.12 nM 7.30
CHEMBL4867905 — IC50 = 63.1 nM 7.20
CHEMBL4858519 — IC50 = 63.1 nM 7.20
CHEMBL4871681 — IC50 = 63.1 nM 7.20
CHEMBL4849259 — IC50 = 79.43 nM 7.10
CHEMBL4635134 GSK620 IC50 = 79.43 nM 7.10
CHEMBL4644310 — IC50 = 79.43 nM 7.10
CHEMBL4866464 — IC50 = 100.0 nM 7.00
CHEMBL4876311 — IC50 = 100.0 nM 7.00
CHEMBL4869589 — IC50 = 125.89 nM 6.90
CHEMBL4873232 — IC50 = 125.89 nM 6.90
CHEMBL4869298 — IC50 = 199.53 nM 6.70
CHEMBL4860666 — IC50 = 316.23 nM 6.50
CHEMBL4854196 — IC50 = 398.11 nM 6.40
CHEMBL4854420 — IC50 = 501.19 nM 6.30
CHEMBL4855380 — IC50 = 794.33 nM 6.10
CHEMBL4860153 — IC50 = 1584.89 nM 5.80
CHEMBL4798618 — IC50 = 3162.28 nM 5.50
CHEMBL4867580 — IC50 = 3981.07 nM 5.40
CHEMBL4637442 — IC50 = 7943.28 nM 5.10
CHEMBL4876876 — IC50 = 31622.78 nM 4.50
CHEMBL4859086 — IC50 > 50118.72 nM -