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Assay Detail

CHEMBL4382969

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Binding
Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay
ChEMBL ↗
52
Total Activities
26
Compounds Tested
2
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

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.
Qin C, Hu Y, Zhou B, Fernandez-Salas E, Yang CY, Liu L, McEachern D, Przybranowski S, Wang M, Stuckey J, Meagher J, Bai L, Chen Z, Lin M, Yang J, Ziazadeh DN, Xu F, Hu J, Xiang W, Huang L, Li S, Wen B, Sun D, Wang S.
J Med Chem (2018) 61 : 6685 -6704
PubMed 30019901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.92 8.00
Ki 26 7.45 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4544682 — — 2 8.68
CHEMBL4555209 — — 2 8.64
CHEMBL4463778 — — 2 8.57
CHEMBL4452894 — — 2 8.43
CHEMBL4532913 — — 2 8.38
CHEMBL1957266 — — 2 8.28
CHEMBL3581647 BIRABRESIB 2.0 2 8.24
CHEMBL4458148 — — 2 8.02
CHEMBL4441402 — — 2 8.02
CHEMBL4464152 — — 2 7.89
CHEMBL4440466 — — 2 7.89
CHEMBL4556533 — — 2 7.82
CHEMBL4439187 — — 2 7.70
CHEMBL4536208 — — 2 7.55
CHEMBL4562288 — — 2 7.48
CHEMBL4459071 — — 2 7.18
CHEMBL4541865 — — 2 7.17
CHEMBL4544722 — — 2 7.17
CHEMBL4449965 — — 2 7.16
CHEMBL4435128 — — 2 7.04
CHEMBL4526981 — — 2 6.72
CHEMBL4583994 — — 2 6.60
CHEMBL4460105 — — 2 6.09
CHEMBL4453137 — — 2 5.82
CHEMBL4475739 — — 2 5.55
CHEMBL4534557 — — 2 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4544682 — Ki = 2.1 nM 8.68
CHEMBL4555209 — Ki = 2.3 nM 8.64
CHEMBL4463778 — Ki = 2.7 nM 8.57
CHEMBL4452894 — Ki = 3.7 nM 8.43
CHEMBL4532913 — Ki = 4.2 nM 8.38
CHEMBL1957266 — Ki = 5.3 nM 8.28
CHEMBL3581647 BIRABRESIB Ki = 5.7 nM 8.24
CHEMBL4441402 — Ki = 9.6 nM 8.02
CHEMBL4458148 — Ki = 9.5 nM 8.02
CHEMBL4555209 — IC50 = 10.0 nM 8.00
CHEMBL4544682 — IC50 = 11.0 nM 7.96
CHEMBL4464152 — Ki = 13.0 nM 7.89
CHEMBL4440466 — Ki = 13.0 nM 7.89
CHEMBL4463778 — IC50 = 13.0 nM 7.89
CHEMBL4532913 — IC50 = 14.0 nM 7.85
CHEMBL4556533 — Ki = 15.0 nM 7.82
CHEMBL4452894 — IC50 = 18.0 nM 7.75
CHEMBL4439187 — Ki = 20.0 nM 7.70
CHEMBL1957266 — IC50 = 22.0 nM 7.66
CHEMBL3581647 BIRABRESIB IC50 = 23.0 nM 7.64
CHEMBL4536208 — Ki = 28.0 nM 7.55
CHEMBL4562288 — Ki = 33.0 nM 7.48
CHEMBL4441402 — IC50 = 34.0 nM 7.47
CHEMBL4458148 — IC50 = 34.0 nM 7.47
CHEMBL4440466 — IC50 = 44.0 nM 7.36
CHEMBL4464152 — IC50 = 45.0 nM 7.35
CHEMBL4556533 — IC50 = 50.0 nM 7.30
CHEMBL4439187 — IC50 = 63.0 nM 7.20
CHEMBL4459071 — Ki = 66.0 nM 7.18
CHEMBL4544722 — Ki = 68.0 nM 7.17
CHEMBL4541865 — Ki = 68.0 nM 7.17
CHEMBL4449965 — Ki = 70.0 nM 7.16
CHEMBL4536208 — IC50 = 86.0 nM 7.07
CHEMBL4435128 — Ki = 92.0 nM 7.04
CHEMBL4562288 — IC50 = 100.0 nM 7.00
CHEMBL4526981 — Ki = 190.0 nM 6.72
CHEMBL4541865 — IC50 = 200.0 nM 6.70
CHEMBL4459071 — IC50 = 200.0 nM 6.70
CHEMBL4544722 — IC50 = 200.0 nM 6.70
CHEMBL4449965 — IC50 = 210.0 nM 6.68
CHEMBL4583994 — Ki = 250.0 nM 6.60
CHEMBL4435128 — IC50 = 270.0 nM 6.57
CHEMBL4526981 — IC50 = 550.0 nM 6.26
CHEMBL4583994 — IC50 = 720.0 nM 6.14
CHEMBL4460105 — Ki = 820.0 nM 6.09
CHEMBL4453137 — Ki = 1500.0 nM 5.82
CHEMBL4460105 — IC50 = 2300.0 nM 5.64
CHEMBL4475739 — Ki = 2800.0 nM 5.55
CHEMBL4534557 — Ki = 3300.0 nM 5.48
CHEMBL4453137 — IC50 = 4400.0 nM 5.36