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Assay Detail

CHEMBL4325264

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

Binding
Inhibition of PI3Kdelta in human whole blood assessed as reduction in cytostim-stimulated IFNgamma production preincubated for 1 hr followed by cytostim stimulation and measured after 20 hrs by electrochemiluminescence assay
ChEMBL ↗
40
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD, Grandi P, Gore PM, Keeling S, Livia S, Mallett D, Maxwell A, Price M, Rau C, Reinhard FBM, Rowedder J, Rowland P, Taylor JA, Thomas DA, Hessel EM, Hamblin JN.
J Med Chem (2020) 63 : 638 -655
PubMed 31855425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.60 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4567736 — — 1 8.10
CHEMBL4449047 — — 1 7.60
CHEMBL4545906 — — 1 7.60
CHEMBL4556087 — — 1 7.50
CHEMBL4538635 — — 1 7.40
CHEMBL4466265 — — 1 7.40
CHEMBL4553962 — — 1 7.30
CHEMBL4579923 — — 1 7.20
CHEMBL4448491 — — 1 7.10
CHEMBL4518946 — — 1 7.10
CHEMBL4444082 — — 2 7.10
CHEMBL4561242 — — 1 7.10
CHEMBL4436797 — — 1 7.10
CHEMBL4467361 — — 1 6.90
CHEMBL4447804 — — 1 6.80
CHEMBL4519361 — — 1 6.60
CHEMBL4462123 — — 1 6.60
CHEMBL4580593 — — 1 6.60
CHEMBL4582886 — — 1 6.50
CHEMBL4533741 — — 1 6.50
CHEMBL4436659 — — 1 6.50
CHEMBL4521647 — — 1 6.40
CHEMBL4453668 — — 1 6.40
CHEMBL4560410 — — 1 6.30
CHEMBL4472036 — — 1 6.30
CHEMBL4518196 — — 1 6.30
CHEMBL4554783 — — 1 6.30
CHEMBL4467351 — — 1 6.30
CHEMBL4580436 — — 1 6.20
CHEMBL4472815 — — 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4567736 — IC50 = 7.943 nM 8.10
CHEMBL4545906 — IC50 = 25.12 nM 7.60
CHEMBL4449047 — IC50 = 25.12 nM 7.60
CHEMBL4556087 — IC50 = 31.62 nM 7.50
CHEMBL4466265 — IC50 = 39.81 nM 7.40
CHEMBL4538635 — IC50 = 39.81 nM 7.40
CHEMBL4553962 — IC50 = 50.12 nM 7.30
CHEMBL4579923 — IC50 = 63.1 nM 7.20
CHEMBL4436797 — IC50 = 79.43 nM 7.10
CHEMBL4448491 — IC50 = 79.43 nM 7.10
CHEMBL4518946 — IC50 = 79.43 nM 7.10
CHEMBL4444082 — IC50 = 79.43 nM 7.10
CHEMBL4561242 — IC50 = 79.43 nM 7.10
CHEMBL4467361 — IC50 = 125.89 nM 6.90
CHEMBL4447804 — IC50 = 158.49 nM 6.80
CHEMBL4444082 — IC50 = 199.53 nM 6.70
CHEMBL4462123 — IC50 = 251.19 nM 6.60
CHEMBL4519361 — IC50 = 251.19 nM 6.60
CHEMBL4580593 — IC50 = 251.19 nM 6.60
CHEMBL4436659 — IC50 = 316.23 nM 6.50
CHEMBL4533741 — IC50 = 316.23 nM 6.50
CHEMBL4582886 — IC50 = 316.23 nM 6.50
CHEMBL4521647 — IC50 = 398.11 nM 6.40
CHEMBL4453668 — IC50 = 398.11 nM 6.40
CHEMBL4560410 — IC50 = 501.19 nM 6.30
CHEMBL4472036 — IC50 = 501.19 nM 6.30
CHEMBL4518196 — IC50 = 501.19 nM 6.30
CHEMBL4554783 — IC50 = 501.19 nM 6.30
CHEMBL4467351 — IC50 = 501.19 nM 6.30
CHEMBL4472815 — IC50 = 630.96 nM 6.20
CHEMBL4580436 — IC50 = 630.96 nM 6.20
CHEMBL4521097 — IC50 = 794.33 nM 6.10
CHEMBL4522200 — IC50 = 1000.0 nM 6.00
CHEMBL4561182 — IC50 = 1000.0 nM 6.00
CHEMBL4466729 — IC50 = 1258.93 nM 5.90
CHEMBL4444773 — IC50 = 1584.89 nM 5.80
CHEMBL4445958 — IC50 = 1995.26 nM 5.70
CHEMBL4457454 — IC50 = 5011.87 nM 5.30
CHEMBL4588903 — IC50 = 19952.62 nM 4.70
CHEMBL4571612 — IC50 > 39810.72 nM -