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Assay Detail

CHEMBL2065220

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

Binding
Inhibition of PI3Kalpha by high throughput chemoproteomics binding assay
ChEMBL ↗
48
Total Activities
48
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

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR studies around a series of triazolopyridines as potent and selective PI3Kγ inhibitors.
Bell K, Sunose M, Ellard K, Cansfield A, Taylor J, Miller W, Ramsden N, Bergamini G, Neubauer G.
Bioorg Med Chem Lett (2012) 22 : 5257 -5263
PubMed 22819766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 5.51 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064508 — — 1 6.80
CHEMBL2064498 — — 1 6.70
CHEMBL2064482 — — 1 6.50
CHEMBL2064495 — — 1 5.80
CHEMBL2059909 — — 1 5.60
CHEMBL2064511 — — 1 5.60
CHEMBL2064512 — — 1 5.50
CHEMBL2064509 — — 1 5.40
CHEMBL2059907 — — 1 5.40
CHEMBL2064484 — — 1 5.30
CHEMBL2064496 — — 1 5.20
CHEMBL2059908 — — 1 5.00
CHEMBL2064489 — — 1 5.00
CHEMBL2064479 — — 1 4.90
CHEMBL2064492 — — 1 4.80
CHEMBL2064481 — — 1 4.60
CHEMBL2064572 — — 1 -
CHEMBL2064513 — — 1 -
CHEMBL2064514 — — 1 -
CHEMBL2064566 — — 1 -
CHEMBL2064567 — — 1 -
CHEMBL2064568 — — 1 -
CHEMBL2064569 — — 1 -
CHEMBL2064510 — — 1 -
CHEMBL2064570 — — 1 -
CHEMBL2064571 — — 1 -
CHEMBL2064478 — — 1 -
CHEMBL2064507 — — 1 -
CHEMBL2064506 — — 1 -
CHEMBL2064505 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064508 — IC50 = 158.49 nM 6.80
CHEMBL2064498 — IC50 = 199.53 nM 6.70
CHEMBL2064482 — IC50 = 316.23 nM 6.50
CHEMBL2064495 — IC50 = 1584.89 nM 5.80
CHEMBL2059909 — IC50 = 2511.89 nM 5.60
CHEMBL2064511 — IC50 = 2511.89 nM 5.60
CHEMBL2064512 — IC50 = 3162.28 nM 5.50
CHEMBL2064509 — IC50 = 3981.07 nM 5.40
CHEMBL2059907 — IC50 = 3981.07 nM 5.40
CHEMBL2064484 — IC50 = 5011.87 nM 5.30
CHEMBL2064496 — IC50 = 6309.57 nM 5.20
CHEMBL2059908 — IC50 = 10000.0 nM 5.00
CHEMBL2064489 — IC50 = 10000.0 nM 5.00
CHEMBL2064479 — IC50 = 12589.25 nM 4.90
CHEMBL2064492 — IC50 = 15848.93 nM 4.80
CHEMBL2064481 — IC50 = 25118.86 nM 4.60
CHEMBL2064483 — IC50 > 50118.72 nM -
CHEMBL2064485 — IC50 > 10000.0 nM -
CHEMBL2064486 — IC50 > 50118.72 nM -
CHEMBL2064487 — IC50 > 100000.0 nM -
CHEMBL2064488 — IC50 > 100000.0 nM -
CHEMBL2064490 — IC50 > 100000.0 nM -
CHEMBL2064491 — IC50 > 19952.62 nM -
CHEMBL2064504 — IC50 > 3981.07 nM -
CHEMBL2064493 — IC50 > 15848.93 nM -
CHEMBL2064494 — IC50 > 100000.0 nM -
CHEMBL2064497 — IC50 > 63095.73 nM -
CHEMBL2064499 — IC50 > 3981.07 nM -
CHEMBL2064500 — IC50 > 3162.28 nM -
CHEMBL2064501 — IC50 > 100.0 nM -
CHEMBL2064502 — IC50 > 100000.0 nM -
CHEMBL2064503 — IC50 > 100000.0 nM -
CHEMBL2064480 — IC50 > 79432.82 nM -
CHEMBL2062546 — IC50 > 100000.0 nM -
CHEMBL2064505 — IC50 > 100000.0 nM -
CHEMBL2064506 — IC50 > 100000.0 nM -
CHEMBL2064507 — IC50 > 100.0 nM -
CHEMBL2064478 — IC50 > 100000.0 nM -
CHEMBL2064571 — IC50 > 10000.0 nM -
CHEMBL2064570 — IC50 > 19952.62 nM -
CHEMBL2064510 — IC50 > 19952.62 nM -
CHEMBL2064569 — IC50 > 100000.0 nM -
CHEMBL2064568 — IC50 > 100000.0 nM -
CHEMBL2064567 — IC50 > 100000.0 nM -
CHEMBL2064566 — IC50 > 100000.0 nM -
CHEMBL2064514 — IC50 > 39810.72 nM -
CHEMBL2064513 — IC50 > 15848.93 nM -
CHEMBL2064572 — IC50 > 100000.0 nM -