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Assay Detail

CHEMBL5385396

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

Binding
Inhibition of terbium-labelled Mcl-1 (unknown origin)/Bim BH3 peptide (H3N-(C/Cy5Mal)-WIAQELRRIGDEFN-OH) (unknown origin) interaction assessed as displacement of Cy5-labeled Bim BH3 peptide by TR-HTRF assay
ChEMBL ↗
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Discovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein-Protein Interaction Modulator with the Potential of Treating Hematological Malignancies.
Romanov-Michailidis F, Hsiao CC, Urner LM, Jerhaoui S, Surkyn M, Miller B, Vos A, Dominguez Blanco M, Bueters R, Vinken P, Bekkers M, Walker D, Pietrak B, Eyckmans W, Dores-Sousa JL, Joo Koo S, Lento W, Bauser M, Philippar U, Rombouts FJR.
J Med Chem (2023) 66 : 6122 -6148
PubMed 37114951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 9.84 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410775 — — 1 10.96
CHEMBL5429389 — — 1 10.96
CHEMBL5410847 — — 1 10.85
CHEMBL5401256 — — 1 10.85
CHEMBL5437247 — — 1 10.82
CHEMBL5394218 — — 1 10.64
CHEMBL5427236 — — 1 10.60
CHEMBL4297482 AZD-5991 1.0 1 10.48
CHEMBL4650225 MURIZATOCLAX 1.0 1 10.37
CHEMBL5428598 — — 1 10.32
CHEMBL5409094 — — 1 10.10
CHEMBL5399943 — — 1 10.06
CHEMBL5397451 — — 1 10.02
CHEMBL5424071 — — 1 9.89
CHEMBL5419723 — — 1 9.82
CHEMBL5439337 — — 1 9.77
CHEMBL5407173 — — 1 9.74
CHEMBL5440477 — — 1 9.72
CHEMBL4439276 — — 1 9.70
CHEMBL5423832 — — 1 9.66
CHEMBL5421600 — — 1 9.66
CHEMBL5394906 — — 1 9.64
CHEMBL5440375 — — 1 9.60
CHEMBL4446378 TAPOTOCLAX 1.0 1 9.49
CHEMBL5403591 — — 1 9.33
CHEMBL5430611 — — 1 9.28
CHEMBL5418181 — — 1 9.17
CHEMBL5408787 — — 1 9.14
CHEMBL5440547 — — 1 8.95
CHEMBL5422740 — — 1 8.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410775 — Ki = 0.011 nM 10.96
CHEMBL5429389 — Ki = 0.011 nM 10.96
CHEMBL5410847 — Ki = 0.014 nM 10.85
CHEMBL5401256 — Ki = 0.014 nM 10.85
CHEMBL5437247 — Ki = 0.015 nM 10.82
CHEMBL5394218 — Ki = 0.023 nM 10.64
CHEMBL5427236 — Ki = 0.025 nM 10.60
CHEMBL4297482 AZD-5991 Ki = 0.033 nM 10.48
CHEMBL4650225 MURIZATOCLAX Ki = 0.043 nM 10.37
CHEMBL5428598 — Ki = 0.048 nM 10.32
CHEMBL5409094 — Ki = 0.08 nM 10.10
CHEMBL5399943 — Ki = 0.088 nM 10.06
CHEMBL5397451 — Ki = 0.096 nM 10.02
CHEMBL5424071 — Ki = 0.13 nM 9.89
CHEMBL5419723 — Ki = 0.15 nM 9.82
CHEMBL5439337 — Ki = 0.17 nM 9.77
CHEMBL5407173 — Ki = 0.18 nM 9.74
CHEMBL5440477 — Ki = 0.19 nM 9.72
CHEMBL4439276 — Ki = 0.2 nM 9.70
CHEMBL5423832 — Ki = 0.22 nM 9.66
CHEMBL5421600 — Ki = 0.22 nM 9.66
CHEMBL5394906 — Ki = 0.23 nM 9.64
CHEMBL5440375 — Ki = 0.25 nM 9.60
CHEMBL4446378 TAPOTOCLAX Ki = 0.32 nM 9.49
CHEMBL5403591 — Ki = 0.47 nM 9.33
CHEMBL5430611 — Ki = 0.52 nM 9.28
CHEMBL5418181 — Ki = 0.67 nM 9.17
CHEMBL5408787 — Ki = 0.72 nM 9.14
CHEMBL5440547 — Ki = 1.13 nM 8.95
CHEMBL5422740 — Ki = 2.36 nM 8.63
CHEMBL5427970 — Ki = 5.1 nM 8.29
CHEMBL5426438 — Ki = 5.29 nM 8.28