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Assay Detail

CHEMBL4672802

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

Binding
Inhibition of recombinant full-length His-tagged human BTK expressed in baculovirus expression system using fluoresceinated peptide as substrate incubated for 60 mins by fluorescence assay
ChEMBL ↗
20
Total Activities
9
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

Tyrosine-protein kinase BTK (CHEMBL5251) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Srivastava AS,Ko S,Watterson SH,Pattoli MA,Skala S,Cheng L,Obermeier MT,Vickery R,Discenza LN,D'Arienzo CJ,Gillooly KM,Taylor TL,Pulicicchio C,McIntyre KW,Yip S,Li P,Sun D,Wu DR,Dai J,Wang C,Zhang Y,Wang B,Pawluczyk J,Kempson J,Zhao R,Hou X,Rampulla R,Mathur A,Galella MA,Salter-Cid L,Barrish JC,Carter PH,Fura A,Burke JR,Tino JA
ACS Med Chem Lett (2020) 11 : 2195 -2203
PubMed 33214829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.85 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891545 — — 4 9.72
CHEMBL3928976 — — 4 9.59
CHEMBL4751952 — — 3 9.39
CHEMBL4741099 — — 1 9.31
CHEMBL4754459 — — 1 9.28
CHEMBL4789404 — — 1 9.20
CHEMBL4743497 — — 3 9.07
CHEMBL4741884 — — 2 8.77
CHEMBL3918580 — — 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891545 — IC50 = 0.19 nM 9.72
CHEMBL3891545 — IC50 = 0.22 nM 9.66
CHEMBL3928976 — IC50 = 0.26 nM 9.59
CHEMBL4751952 — IC50 = 0.41 nM 9.39
CHEMBL4741099 — IC50 = 0.49 nM 9.31
CHEMBL4754459 — IC50 = 0.52 nM 9.28
CHEMBL3928976 — IC50 = 0.55 nM 9.26
CHEMBL4789404 — IC50 = 0.63 nM 9.20
CHEMBL4743497 — IC50 = 0.86 nM 9.07
CHEMBL4751952 — IC50 = 0.94 nM 9.03
CHEMBL4751952 — IC50 = 1.0 nM 9.00
CHEMBL4743497 — IC50 = 1.2 nM 8.92
CHEMBL4743497 — IC50 = 1.7 nM 8.77
CHEMBL4741884 — IC50 = 1.7 nM 8.77
CHEMBL4741884 — IC50 = 1.8 nM 8.74
CHEMBL3918580 — IC50 = 3.0 nM 8.52
CHEMBL3891545 — IC50 = 6.3 nM 8.20
CHEMBL3891545 — IC50 = 7.2 nM 8.14
CHEMBL3928976 — IC50 = 17.0 nM 7.77
CHEMBL3928976 — IC50 = 180.0 nM 6.75