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Assay Detail

CHEMBL4625970

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) BD2 domain Y390A 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 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
Seal JT, Atkinson SJ, Aylott H, Bamborough P, Chung CW, Copley RCB, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Lindon M, Messenger C, Michon AM, Mitchell D, Preston A, Prinjha RK, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH.
J Med Chem (2020) 63 : 9093 -9126
PubMed 32702236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.57 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4646820 — — 1 7.80
CHEMBL4648431 — — 1 7.80
CHEMBL4641088 — — 1 7.70
CHEMBL4638062 — — 1 7.30
CHEMBL4636881 GSK046 — 1 7.30
CHEMBL4637851 — — 1 7.20
CHEMBL4635355 — — 1 7.20
CHEMBL4634679 — — 1 7.20
CHEMBL4645843 — — 1 7.10
CHEMBL4637489 — — 1 7.10
CHEMBL4644310 — — 1 7.10
CHEMBL4635134 GSK620 — 1 7.10
CHEMBL4638988 — — 1 7.00
CHEMBL4638747 — — 1 7.00
CHEMBL4634311 — — 1 7.00
CHEMBL4641419 — — 1 7.00
CHEMBL4641442 — — 1 7.00
CHEMBL4637791 — — 1 7.00
CHEMBL4642732 — — 1 6.90
CHEMBL4646106 — — 1 6.90
CHEMBL4633616 — — 1 6.90
CHEMBL4635674 — — 1 6.90
CHEMBL4634917 — — 1 6.90
CHEMBL4633275 — — 1 6.80
CHEMBL4636094 — — 1 6.80
CHEMBL4649888 — — 1 6.80
CHEMBL4643683 — — 1 6.80
CHEMBL4643238 — — 1 6.70
CHEMBL4643352 — — 1 6.70
CHEMBL4635406 — — 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4646820 — IC50 = 15.85 nM 7.80
CHEMBL4648431 — IC50 = 15.85 nM 7.80
CHEMBL4641088 — IC50 = 19.95 nM 7.70
CHEMBL4638062 — IC50 = 50.12 nM 7.30
CHEMBL4636881 GSK046 IC50 = 50.12 nM 7.30
CHEMBL4637851 — IC50 = 63.1 nM 7.20
CHEMBL4635355 — IC50 = 63.1 nM 7.20
CHEMBL4634679 — IC50 = 63.1 nM 7.20
CHEMBL4645843 — IC50 = 79.43 nM 7.10
CHEMBL4637489 — IC50 = 79.43 nM 7.10
CHEMBL4644310 — IC50 = 79.43 nM 7.10
CHEMBL4635134 GSK620 IC50 = 79.43 nM 7.10
CHEMBL4641442 — IC50 = 100.0 nM 7.00
CHEMBL4638747 — IC50 = 100.0 nM 7.00
CHEMBL4634311 — IC50 = 100.0 nM 7.00
CHEMBL4638988 — IC50 = 100.0 nM 7.00
CHEMBL4641419 — IC50 = 100.0 nM 7.00
CHEMBL4637791 — IC50 = 100.0 nM 7.00
CHEMBL4642732 — IC50 = 125.89 nM 6.90
CHEMBL4646106 — IC50 = 125.89 nM 6.90
CHEMBL4633616 — IC50 = 125.89 nM 6.90
CHEMBL4635674 — IC50 = 125.89 nM 6.90
CHEMBL4634917 — IC50 = 125.89 nM 6.90
CHEMBL4643683 — IC50 = 158.49 nM 6.80
CHEMBL4636094 — IC50 = 158.49 nM 6.80
CHEMBL4633275 — IC50 = 158.49 nM 6.80
CHEMBL4649888 — IC50 = 158.49 nM 6.80
CHEMBL4643238 — IC50 = 199.53 nM 6.70
CHEMBL4643352 — IC50 = 199.53 nM 6.70
CHEMBL4635406 — IC50 = 251.19 nM 6.60
CHEMBL4642067 — IC50 = 251.19 nM 6.60
CHEMBL4649746 — IC50 = 398.11 nM 6.40
CHEMBL4635275 — IC50 = 398.11 nM 6.40
CHEMBL4649837 — IC50 = 501.19 nM 6.30
CHEMBL4645874 — IC50 = 630.96 nM 6.20
CHEMBL4638355 — IC50 = 630.96 nM 6.20
CHEMBL4643576 — IC50 = 630.96 nM 6.20
CHEMBL4637823 — IC50 = 794.33 nM 6.10
CHEMBL4638058 — IC50 = 1000.0 nM 6.00
CHEMBL4649033 — IC50 = 1258.93 nM 5.90
CHEMBL4633353 — IC50 = 1258.93 nM 5.90
CHEMBL4647845 — IC50 = 1995.26 nM 5.70
CHEMBL4644967 — IC50 = 2511.89 nM 5.60
CHEMBL4645221 — IC50 = 2511.89 nM 5.60
CHEMBL4645180 — IC50 = 3162.28 nM 5.50
CHEMBL4639935 — IC50 = 6309.57 nM 5.20
CHEMBL4637442 — IC50 = 7943.28 nM 5.10
CHEMBL4639878 — IC50 = 12589.25 nM 4.90
CHEMBL4634393 — IC50 = 25118.86 nM 4.60