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Assay Detail

CHEMBL3427871

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

Functional
Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay
ChEMBL ↗
87
Total Activities
45
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

Publication

Removal of Metabolic Liabilities Enables Development of Derivatives of Procaspase-Activating Compound 1 (PAC-1) with Improved Pharmacokinetics.
Roth HS, Botham RC, Schmid SC, Fan TM, Dirikolu L, Hergenrother PJ.
J Med Chem (2015) 58 : 4046 -4065
PubMed 25856364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.05 5.47
Activity 42 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426434 — — 2 5.47
CHEMBL3426443 — — 2 5.41
CHEMBL3426417 — — 2 5.39
CHEMBL3426425 — — 2 5.33
CHEMBL3425520 — — 2 5.32
CHEMBL3426411 — — 2 5.31
CHEMBL3426444 — — 2 5.28
CHEMBL3426435 — — 2 5.19
CHEMBL3426409 — — 2 5.18
CHEMBL3426416 — — 2 5.14
CHEMBL3426442 — — 2 5.12
CHEMBL3426441 — — 2 5.12
CHEMBL3426429 — — 2 5.07
CHEMBL3426433 — — 2 5.07
CHEMBL3426437 — — 2 5.06
CHEMBL3426426 — — 2 5.06
CHEMBL3426413 — — 2 5.05
CHEMBL3426436 — — 2 5.05
CHEMBL3426403 — — 2 5.05
CHEMBL3426440 — — 2 5.03
CHEMBL3426412 — — 2 5.03
CHEMBL3426410 — — 2 5.02
CHEMBL3426427 — — 2 5.02
CHEMBL3426428 — — 2 5.01
CHEMBL3426431 — — 2 5.00
CHEMBL3426415 — — 2 5.00
CHEMBL591429 PAC-1 1.0 2 4.99
CHEMBL3426432 — — 2 4.99
CHEMBL3426407 — — 2 4.99
CHEMBL583789 — — 2 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426434 — IC50 = 3400.0 nM 5.47
CHEMBL3426443 — IC50 = 3900.0 nM 5.41
CHEMBL3426417 — IC50 = 4100.0 nM 5.39
CHEMBL3426425 — IC50 = 4700.0 nM 5.33
CHEMBL3425520 — IC50 = 4800.0 nM 5.32
CHEMBL3426411 — IC50 = 4900.0 nM 5.31
CHEMBL3426444 — IC50 = 5200.0 nM 5.28
CHEMBL3426435 — IC50 = 6500.0 nM 5.19
CHEMBL3426409 — IC50 = 6600.0 nM 5.18
CHEMBL3426416 — IC50 = 7300.0 nM 5.14
CHEMBL3426442 — IC50 = 7500.0 nM 5.12
CHEMBL3426441 — IC50 = 7500.0 nM 5.12
CHEMBL3426433 — IC50 = 8500.0 nM 5.07
CHEMBL3426429 — IC50 = 8600.0 nM 5.07
CHEMBL3426437 — IC50 = 8700.0 nM 5.06
CHEMBL3426426 — IC50 = 8700.0 nM 5.06
CHEMBL3426413 — IC50 = 9000.0 nM 5.05
CHEMBL3426403 — IC50 = 8900.0 nM 5.05
CHEMBL3426436 — IC50 = 8900.0 nM 5.05
CHEMBL3426412 — IC50 = 9400.0 nM 5.03
CHEMBL3426440 — IC50 = 9400.0 nM 5.03
CHEMBL3426410 — IC50 = 9600.0 nM 5.02
CHEMBL3426427 — IC50 = 9500.0 nM 5.02
CHEMBL3426428 — IC50 = 9800.0 nM 5.01
CHEMBL3426415 — IC50 = 10000.0 nM 5.00
CHEMBL3426431 — IC50 = 10100.0 nM 5.00
CHEMBL3426432 — IC50 = 10300.0 nM 4.99
CHEMBL3426407 — IC50 = 10200.0 nM 4.99
CHEMBL591429 PAC-1 IC50 = 10200.0 nM 4.99
CHEMBL583789 — IC50 = 11100.0 nM 4.96
CHEMBL3426439 — IC50 = 11200.0 nM 4.95
CHEMBL3426404 — IC50 = 12100.0 nM 4.92
CHEMBL3426438 — IC50 = 12300.0 nM 4.91
CHEMBL3426430 — IC50 = 12700.0 nM 4.90
CHEMBL3426414 — IC50 = 12800.0 nM 4.89
CHEMBL3426406 — IC50 = 13100.0 nM 4.88
CHEMBL3426405 — IC50 = 13700.0 nM 4.86
CHEMBL3426408 — IC50 = 15300.0 nM 4.82
CHEMBL3426424 — IC50 = 15300.0 nM 4.82
CHEMBL3426422 — IC50 = 15300.0 nM 4.82
CHEMBL3426420 — IC50 = 15700.0 nM 4.80
CHEMBL3426418 — IC50 = 17000.0 nM 4.77
CHEMBL3426435 — Activity - — -
CHEMBL3426422 — Activity - — -
CHEMBL3426424 — Activity - — -
CHEMBL3426425 — Activity - — -
CHEMBL3426426 — Activity - — -
CHEMBL3426427 — Activity - — -
CHEMBL3426428 — Activity - — -
CHEMBL3426429 — Activity - — -