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Assay Detail

CHEMBL4835098

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

Binding
Inhibition of 6His-Thr-BRD4 (1 to 477 residues) BD2 domain Y390A mutant (unknown origin) incubated for 30 mins by TR-FRET assay
ChEMBL ↗
51
Total Activities
51
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

Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Aylott HE, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Seal JT, Wall ID, Watson RJ, Woolven JM, Demont EH.
J Med Chem (2021) 64 : 3249 -3281
PubMed 33662213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.60 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4858925 — — 1 8.00
CHEMBL4863802 — — 1 8.00
CHEMBL4847219 — — 1 7.60
CHEMBL4855180 — — 1 7.60
CHEMBL4858325 — — 1 7.60
CHEMBL4878969 — — 1 7.60
CHEMBL4856853 — — 1 7.50
CHEMBL4862336 — — 1 7.50
CHEMBL4871396 — — 1 7.40
CHEMBL4636881 GSK046 — 1 7.30
CHEMBL4867703 — — 1 7.30
CHEMBL4848118 — — 1 7.30
CHEMBL4869949 — — 1 7.20
CHEMBL4876163 — — 1 7.20
CHEMBL4635134 GSK620 — 1 7.10
CHEMBL4877538 — — 1 7.10
CHEMBL4859566 — — 1 7.00
CHEMBL4853265 — — 1 6.90
CHEMBL4860289 — — 1 6.90
CHEMBL4855237 — — 1 6.90
CHEMBL4866042 — — 1 6.90
CHEMBL4858948 — — 1 6.90
CHEMBL4855487 — — 1 6.90
CHEMBL4867905 — — 1 6.80
CHEMBL4872640 — — 1 6.70
CHEMBL4863181 — — 1 6.70
CHEMBL4864664 — — 1 6.60
CHEMBL4851002 — — 1 6.60
CHEMBL4858046 — — 1 6.60
CHEMBL4863490 — — 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4858925 — IC50 = 10.0 nM 8.00
CHEMBL4863802 — IC50 = 10.0 nM 8.00
CHEMBL4855180 — IC50 = 25.12 nM 7.60
CHEMBL4858325 — IC50 = 25.12 nM 7.60
CHEMBL4878969 — IC50 = 25.12 nM 7.60
CHEMBL4847219 — IC50 = 25.12 nM 7.60
CHEMBL4856853 — IC50 = 31.62 nM 7.50
CHEMBL4862336 — IC50 = 31.62 nM 7.50
CHEMBL4871396 — IC50 = 39.81 nM 7.40
CHEMBL4636881 GSK046 IC50 = 50.12 nM 7.30
CHEMBL4867703 — IC50 = 50.12 nM 7.30
CHEMBL4848118 — IC50 = 50.12 nM 7.30
CHEMBL4876163 — IC50 = 63.1 nM 7.20
CHEMBL4869949 — IC50 = 63.1 nM 7.20
CHEMBL4877538 — IC50 = 79.43 nM 7.10
CHEMBL4635134 GSK620 IC50 = 79.43 nM 7.10
CHEMBL4859566 — IC50 = 100.0 nM 7.00
CHEMBL4853265 — IC50 = 125.89 nM 6.90
CHEMBL4860289 — IC50 = 125.89 nM 6.90
CHEMBL4855237 — IC50 = 125.89 nM 6.90
CHEMBL4866042 — IC50 = 125.89 nM 6.90
CHEMBL4858948 — IC50 = 125.89 nM 6.90
CHEMBL4855487 — IC50 = 125.89 nM 6.90
CHEMBL4867905 — IC50 = 158.49 nM 6.80
CHEMBL4863181 — IC50 = 199.53 nM 6.70
CHEMBL4872640 — IC50 = 199.53 nM 6.70
CHEMBL4864664 — IC50 = 251.19 nM 6.60
CHEMBL4851002 — IC50 = 251.19 nM 6.60
CHEMBL4858046 — IC50 = 251.19 nM 6.60
CHEMBL4863490 — IC50 = 251.19 nM 6.60
CHEMBL4853673 — IC50 = 251.19 nM 6.60
CHEMBL4856289 — IC50 = 251.19 nM 6.60
CHEMBL4878769 — IC50 = 316.23 nM 6.50
CHEMBL4853894 — IC50 = 316.23 nM 6.50
CHEMBL4857257 — IC50 = 316.23 nM 6.50
CHEMBL4863257 — IC50 = 398.11 nM 6.40
CHEMBL4856303 — IC50 = 501.19 nM 6.30
CHEMBL4857786 — IC50 = 630.96 nM 6.20
CHEMBL4854847 — IC50 = 794.33 nM 6.10
CHEMBL4858315 — IC50 = 1000.0 nM 6.00
CHEMBL4869110 — IC50 = 1000.0 nM 6.00
CHEMBL4868943 — IC50 = 1584.89 nM 5.80
CHEMBL4863202 — IC50 = 1584.89 nM 5.80
CHEMBL4872621 — IC50 = 2511.89 nM 5.60
CHEMBL4876704 — IC50 = 3981.07 nM 5.40
CHEMBL4861178 — IC50 = 3981.07 nM 5.40
CHEMBL4851810 — IC50 = 7943.28 nM 5.10
CHEMBL4854063 — IC50 = 10000.0 nM 5.00
CHEMBL4878676 — IC50 = 12589.25 nM 4.90
CHEMBL4845885 — IC50 = 15848.93 nM 4.80