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Assay Detail

CHEMBL700213

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

Functional
Inhibitory concentration against human K562 leukemia cells following incubation for 1 hour
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K562
Confidence 1 — Organism
Curated By Intermediate

Target

K562 (CHEMBL385)
Type CELL-LINE
Organism Homo sapiens

Publication

Linker length modulates DNA cross-linking reactivity and cytotoxic potency of C8/C8' ether-linked C2-exo-unsaturated pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimers.
Gregson SJ, Howard PW, Gullick DR, Hamaguchi A, Corcoran KE, Brooks NA, Hartley JA, Jenkins TC, Patel S, Guille MJ, Thurston DE.
J Med Chem (2004) 47 : 1161 -1174
PubMed 14971896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.79 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16498 SJG-136 2.0 1 7.37
CHEMBL279754 DSB-120 1 6.70
CHEMBL17005 1 6.30
CHEMBL16932 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16498 SJG-136 IC50 = 43.0 nM 7.37
CHEMBL279754 DSB-120 IC50 = 200.0 nM 6.70
CHEMBL17005 IC50 = 500.0 nM 6.30
CHEMBL16932 IC50 < 1.0 nM -