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Assay Detail

CHEMBL5226216

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

Functional
Antiproliferative activity against human KARPAS-422 cell assessed as cell growth inhibition incubated for 6 days by ATPlite reagent based luminescence assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KARPAS-422
Confidence 1 — Organism
Curated By Autocuration

Target

KARPAS-422 (CHEMBL2366368)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
Mamai A, Chau AM, Wilson BJ, Watson ID, Joseph BB, Subramanian PR, Morshed MM, Morin JA, Prakesch MA, Lu T, Connolly P, Kuntz DA, Pomroy NC, Poda G, Nguyen K, Marcellus R, Strathdee G, Theriault B, Subramaniam R, Mohammed M, Abibi A, Chan M, Winston J, Kiyota T, Undzys E, Aman A, Austin N, Du Jardin M, Packman K, Phillippar U, Attar R, Edwards J, O'Meara J, Uehling DE, Al-Awar R, Privé GG, Isaac MB.
ACS Med Chem Lett (2023) 14 : 199 -210
PubMed 36793435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.57 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5282647 1 8.05
CHEMBL5283745 1 7.89
CHEMBL5270031 1 7.58
CHEMBL5285804 1 7.19
CHEMBL5275407 1 7.07
CHEMBL5279363 1 7.04
CHEMBL5269780 1 6.99
CHEMBL5287446 1 6.92
CHEMBL5288796 1 6.86
CHEMBL5285971 1 6.85
CHEMBL5269124 1 6.82
CHEMBL5279982 1 6.79
CHEMBL5291358 1 6.78
CHEMBL5288047 1 6.70
CHEMBL5271863 1 6.70
CHEMBL5271784 1 6.68
CHEMBL5287071 1 6.64
CHEMBL5271042 1 6.57
CHEMBL5268066 1 6.52
CHEMBL5291478 1 6.39
CHEMBL5290428 1 6.36
CHEMBL5272054 1 6.34
CHEMBL5276120 1 6.21
CHEMBL5271895 1 6.19
CHEMBL5285053 1 6.11
CHEMBL5267067 1 6.10
CHEMBL5279858 1 6.01
CHEMBL5279299 1 5.96
CHEMBL5284699 1 5.96
CHEMBL5267621 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5282647 IC50 = 9.0 nM 8.05
CHEMBL5283745 IC50 = 13.0 nM 7.89
CHEMBL5270031 IC50 = 26.0 nM 7.58
CHEMBL5285804 IC50 = 65.0 nM 7.19
CHEMBL5275407 IC50 = 86.0 nM 7.07
CHEMBL5279363 IC50 = 92.0 nM 7.04
CHEMBL5269780 IC50 = 102.0 nM 6.99
CHEMBL5287446 IC50 = 119.0 nM 6.92
CHEMBL5288796 IC50 = 139.0 nM 6.86
CHEMBL5285971 IC50 = 142.0 nM 6.85
CHEMBL5269124 IC50 = 152.0 nM 6.82
CHEMBL5279982 IC50 = 162.0 nM 6.79
CHEMBL5291358 IC50 = 166.0 nM 6.78
CHEMBL5288047 IC50 = 202.0 nM 6.70
CHEMBL5271863 IC50 = 202.0 nM 6.70
CHEMBL5271784 IC50 = 207.0 nM 6.68
CHEMBL5287071 IC50 = 231.0 nM 6.64
CHEMBL5271042 IC50 = 270.0 nM 6.57
CHEMBL5268066 IC50 = 299.0 nM 6.52
CHEMBL5291478 IC50 = 407.0 nM 6.39
CHEMBL5290428 IC50 = 439.0 nM 6.36
CHEMBL5272054 IC50 = 457.0 nM 6.34
CHEMBL5276120 IC50 = 612.0 nM 6.21
CHEMBL5271895 IC50 = 644.0 nM 6.19
CHEMBL5285053 IC50 = 781.0 nM 6.11
CHEMBL5267067 IC50 = 796.0 nM 6.10
CHEMBL5279858 IC50 = 971.0 nM 6.01
CHEMBL5279299 IC50 = 1100.0 nM 5.96
CHEMBL5284699 IC50 = 1100.0 nM 5.96
CHEMBL5267621 IC50 = 1200.0 nM 5.92
CHEMBL5286712 IC50 = 1300.0 nM 5.89
CHEMBL5286263 IC50 = 3200.0 nM 5.50
CHEMBL5284819 IC50 = 7800.0 nM 5.11
CHEMBL5267171 IC50 > 10000.0 nM -